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Award & Prize Lectures
Professor Dr. François Diederich, Laboratory of Organic Chemistry, ETH Zurich, Switzerland.
Research fields: (i) molecular recognition studies with chemical and biological systems to quantify weak intermolecular interactions, (ii) structure-based design of nonpeptidic enzyme inhibitors, and (iii) carbon-rich optoelectronic and chiroptical materials. Education and former professional experience: born in the Grand-Duchy of Luxembourg, Diederich studied chemistry at the University of Heidelberg (1971-1977). After his doctoral dissertation at the Max-Planck-Institute for Medizinische Forschung in Heidelberg (1977-1979), postdoctoral study at UCLA (1979-1981), and Habilitation in Heidelberg (1981-1985), he joined the Department of Chemistry and Biochemistry at UCLA, where he became Full Professor in 1989. In 1992, he joined ETH Zurich as a Professor of Organic Chemistry. Close window NAUTA AWARD FOR PHARMACOCHEMISTRY
Paul J. Hergenrother is a Professor in the Department of Chemistry at the University of Illinois, Urbana-Champaign, where he holds the Kenneth L. Rinehart Jr. Endowed Chair in Natural Products Chemistry.
His laboratory seeks to use novel small molecules to define new targets for the treatment of cancer and drug resistant bacteria. He is a native of Akron, OH, received his B.S. in Chemistry in 1994 from the University of Notre Dame, his Ph.D. from the University of Texas, Austin in 1999 working with Prof. Stephen F. Martin, and from 1999-2001 he was a American Cancer Society postdoctoral fellow at Harvard University, working in the laboratory of Prof. Stuart L. Schreiber. Close window UCB-EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
Michael J. Sofia, Ph.D. is currently Chief Scientific Officer at Arbutus Biopharma, Inc. a company focused on the discovery and development of therapies to treat hepatitis B. Previously he was CSO and Co-founder of OnCore Biopharma which merged with Tekmira in March 2015 to form Arbutus Biopharma. He also holds a professorship at the Baruch S. Blumberg Institute and an Adjunct Professorship at the Drexel University School of Medicine.
Prior to founding OnCore Biopharma, Mike Sofia was Senior Vice President of Chemistry and Senior Advisor at Gilead Sciences and was Sr. Vice President of Chemistry at Pharmasset, Inc until Pharmasset’s acquisition by Gilead in Jan 2012.
Mike Sofia previously held the positions of Group Director New Leads Chemistry at Bristol-Myers Squibb, Vice President of Research at Intercardia Research Labs (formerly Transcell Technologies) and research positions of increasing responsibility at Eli Lilly & Co. and at the Squibb Institute for Medical Research E. R. Squibb.
Mike Sofia did his postdoctoral training as an NIH fellow at Columbia University and received his Ph.D. in organic chemistry from the University of Illinois, Urbana-Champaign. He earned his B.A. degree in chemistry from Cornell University.
Close window IUPAC-RICHTER PRIZE
Jan Steyaert ir. Ph.D. is a full professor and Francqui Research Professor at the Vrije Universiteit Brussel (VUB). He teaches biochemistry and protein engineering for chemists, biologists and bio-engineers.
Jan Steyaert made his Ph.D. at the protein engineering department of Plant Genetic Systems (currently Bayer Crop science). After a postdoc in the International Livestock Research Institute (Nairobi, Kenya), he joined the laboratory of Structural Biology of Lode Wyns. Skilled in enzymology, structural biology and antibody technology. Experienced in steady state and pre-steady state kinetics, protein expression and purification, spectroscopic techniques, structural biology methods and phage display. He is co-founder of Ablynx (www.ablynx.com) and Agrosafve (www.agrosafve.com), and founder of ConFo Therapeutics (www.confotherapeutics.com), three biotech spin-offs that valorize a unique family of single domain antibodies (nanobodies) derived from camels. Last years, the Steyaert lab pioneered the use of nanobodies for chaperone-assisted X-ray crystallography (www.steyaertlab.eu), aiming at the highest hanging fruits of structural biology including membrane proteins, amyloidogenic proteins, and now also (transient) multiprotein complexes. The elucidation of the first GPCR structures in the agonist-bound active state demonstrate the power of Nanobodies to stabilize G protein coupled receptor conformational states including transmembrane signalling complexes. Recent work focusses on exploiting the conformational complexity of therapeutic targets for Nanobody-enabled drug discovery. Jan Steyaert holds a Ph.D in Bioengineering Sciences from the VUB. He is currently Director of the Structural Biology Brussels lab (VUB), acting Director and group leader of the Structural Biology Research center of the Vlaams Instituut voor Biotechnologie (VIB) and partim CSO of Confotherapeutics. Close window PROUS INSTITUTE-OVERTON AND MEYER AWARD
FOR NEW TECHNOLOGIES IN DRUG DISCOVERY Plenary Lectures
Klaus Bock has a Master degree in Chemical Engineering from the Technical University of Demark (1968) and a PhD in Organic Chemistry from the same University (1970).
He was associate professor in organic chemistry at the Technical University of Denmark from 1970 to 1988. From 1988 he was appointed head and professor of the Chemistry Department of the Carlsberg Laboratory, from 1992 Head of Research at Carlsberg Research Centre on from 2001 to 2007 Executive Vice President for Research of Carlsberg A/S. He has published 260 papers in international journals with referee within the area of analytical and synthetic carbohydrate chemistry with special emphasis of the application of NMR spectroscopy in structural studies of carbohydrate derivatives and their interaction with enzymes. From 2004-2012 chairman of the Danish National Research Foundation, from 2005 to 2014 deputy chairman of the Danish National Advanced Technology Foundation and President of the Danish Academy of Technical Sciences 2009-2011. Chair and champion for ESOF 2014, member of the European Research Council 2013- its vice president 2016-, member of The Standing Selection Committee for Canadian Governments Network of Centers of Excellence 2010. Close window The European Research Council (ERC) and its Support for Medicinal Chemistry
Jeffrey studied chemistry and philosophy at Trinity University in San Antonio, Texas. After PhD studies at the the California Institute of Technology and ETH Zürich, he spent two years in Japan as a JSPS postdoctoral fellow at the Tokyo Institute of Technology. In 2003, he began his independent career in US, at UC-Santa Barbara and then the University of Pennsylvania. In 2010, he moved to the Swiss Federal Institute of Technology (ETH) in Zürich, Switzerland, as a full Professor in the Laboratory of Organic Chemistry. Since 2013, he is also has a satellite lab at the Institute of Transformative bio-Molecules at Nagoya University. His research group works on the development of new reactions and chemical biology, particularly on chemical protein synthesis, bioconjugation, and various other projects on synthetic and medicinal chemistry.
Close window Cross-Coupling Approaches to Saturated N-Heterocycles
Simon Campbell is a synthetic organic chemist who received his PhD from the University of Birmingham in 1965 followed by postdoctoral appointments in Chile and Stanford. From 1969 to 1972, he was Visiting Professor at the Universidade do Sao Paulo in Brazil, and he then joined Pfizer Central Research in Sandwich. Simon retired from Pfizer in 1998 as Senior Vice President for Worldwide Discovery and Medicinals R&D Europe. He has co-authored over 130 publications and patents, and was a key member of the research teams that discovered CarduraTM, NorvascTM, and Viagra.TM
Dr Campbell’s scientific contributions have been recognised by numerous awards including election to FRS (1999), FMed Sci (2002) and he was appointed CBE in 2006 for “Services to Science” followed by a Knighthood in 2015 for “Services to Chemistry” Currently, Sir Simon acts as an independent Scientific Consultant for VCs, Biotech, funding agencies and charities, nationally and internationally. Close window Science, Art and Drug Discovery, a Personal Perspective
Derek Lowe was born in Arkansas, and attended Hendrix College (B.A.), and then Duke University for his PhD (1988).
Afterwards he did a Humboldt Foundation post-doc with Bernd Giese at Darmstadt, and returned to the US to take a job a Schering-Plough.
After eight years there, Derek moved to Bayer (in Connecticut) for ten years, and then in 2007 to Vertex, where he is today with the title of Research Fellow. Derek has worked in several different therapeutic areas over the years, but at Vertex he has focused more on new technologies and the so-called "undruggable" targets. Close window Robotics, Artificial Intelligence, and Medicinal Chemistry: A Look Into the Future
Dario Neri studied Chemistry at the Scuola Normale Superiore of Pisa and earned a PhD in Chemistry at the Swiss Federal Institute of Technology (ETH Zürich), under the supervision of Professor Kurt Wüthrich.
He then performed post-doctoral research at the Medical Research Council Centre in Cambridge (UK), under the supervision of Sir Gregory Winter. He has now been a Professor at the ETH Zürich since 1996. The research of the group Neri focuses on the engineering of therapeutic antibodies for the therapy of cancer and other angiogenesis-related disorders. Other research activities include the chemical proteomic discovery of novel vascular markers of pathology and the development of DNA-encoded chemical libraries. Dario Neri is a co-founder of Philogen (www.philogen.com), a Swiss-Italian biotech company which has brought five antibody-based products into multicenter clinical trials for the therapy of cancer and of rheumatoid arthritis. Dario Neri has published over 300 articles in peer-reviewed scientific journals. He is the recipient of the ISOBM Abbott Prize 2000, of the Amgen-Dompe’ Biotec Award 2000, of the Mangia d’Oro 2001, of the Prous Award 2006 of the European Federation of Medicinal Chemistry, of the Robert-Wenner-Prize 2007 of the Swiss Cancer League, of the SWISS BRIDGE Award 2008, of the Prix Mentzer of the French Medicinal Chemistry Society in 2011, of the Phoenix Prize 2014 and of an ERC Advanced Grant in 2015. Close window DNA-Encoded Chemical Libraries
Tobias Ritter received his undergraduate education in Braunschweig, Germany, Bordeaux, France, Lausanne, Switzerland, and Stanford, US. He has performed undergraduate research with Prof. Barry M. Trost at Stanford, obtained his PhD working with Prof. Erick M. Carreira at ETH Zurich in 2004, and was a postdoc with Prof. Robert H. Grubbs at Caltech. In 2006, Tobias was appointed as Assistant Professor in the Department of Chemistry and Chemical Biology at Harvard, promoted to Associate Professor in 2010, and to Professor of Chemistry and Chemical Biology in 2012. Since 2015 he is director at the Max-Planck-Institut fuer Kohlenforschung in Germany and holds additional faculty appointments at Harvard and Massachusetts General Hospital. The Ritter lab focuses on late-stage fluorination chemistry and catalysis for functionalization of complex small molecules.
Close window Late-Stage Fluorination
Tony is Head of Worldwide Medicinal Chemistry and also serves as interim Chief Scientific Officer for Inflammation & Immunology at Pfizer. Prior to this he was Head of Chemistry and Exploratory Medicinal Sciences in Sandwich from February 2007 and Head of Chemistry from April 2004. Tony joined Pfizer as a Scientist in the Department of Discovery Chemistry at Sandwich in 1992. Over the period of the next 8 years he made a number of contributions to the delivery of development candidates in various projects from within the Sexual Health, Urology, and Gastrointestinal Therapeutic Areas. He was appointed to the post of Manager in 1999 with responsibility for Anti-Infectives Chemistry and played a leading role in the discovery of Maraviroc, a CCR5 antagonist for the treatment of HIV, for which he was awarded the RSC Malcolm Campbell Prize in 2005, and was a co-recipient of the ACS Heroes of Chemistry Prize, the Prix Galien USA and Scrip Awards in 2008 and the PhRMA Discoverers Award in 2010. This period of time also saw Tony leading the team that discovered Lersivirine a new non cross resistant non nucleoside reverse transcriptase inhibitor that is currently in Phase II. In recognition of these achievements Tony was awarded the UCB Ehrlich Prize for excellence in medicinal chemistry by the EFMC in 2010.
Tony received his BSc in 1987 and PhD in 1990 in chemistry from the University of Newcastle upon Tyne, before completing post-doctoral studies with Professor Steven Ley, FRS at Imperial College in London working on the total synthesis of azadirachtin, one of the most complex molecules ever to have been synthesized, and a project that has only recently been completed. Tony has active interests in many areas of medicinal chemistry and has held positions on a number of UK funding council review boards such as the BBSRC and EPSRC. He was elected to EPSRC Council in 2010. Tony is also co-editor in chief of the new RSC journal, Medicinal Chemistry Communications, and was editor of volume 41 of Annual Reports in Medicinal Chemistry in 2006. Tony is an author or inventor on more than 50 scientific publications and patents and has given invited lectures at a number of International Conferences on Medicinal Chemistry. Lastly, Tony is a Visiting Professor at the University of Newcastle upon Tyne. Close window Heterocycles and Medicinal Chemistry: The Importance of Innovative Synthesis Invited Speakers
Peptide Drugs to Target GPCR - State of the Art and Innovative Applications
Carmen Almansa is Chemistry Director at ESTEVE, where she is responsible for the chemistry related R&D activities, involving medicinal, synthetic and analytical chemistry as well as compound management.
Until 2011 served as Head of Drug Discovery Outsourcing at Palau Pharma (2008-2010) and team leader in the Medicinal Chemistry department of Grupo Uriach (1989-2007), leading different drug discovery programs that allowed the identification of several development candidates, such as cimicoxib, a COX-2 inhibitor marketed for the treatment of inflammatory pain in animals (Cimalgex, Vetoquinol). She is coauthor of more than 90 international patents, 30 publications in peer-reviewed journals of Organic and Medicinal Chemistry and 30 communications to international congresses, in the cardiovascular, immunology, pain and inflammation fields. Close window Challenges in the Discovery of Sigma-1 Receptor Antagonists for the Treatment of Pain
Since 2012 Dr Baell has been a research professor in medicinal chemistry at the Monash Institute of Pharmaceutical Sciences (MIPS), Monash University, Australia, and co-director of the Australian Translational Medicinal Chemistry Facility.
He obtained his PhD from the Victorian College of Pharmacy (Peter Andrews/Paul Alewood), University of Melbourne in 1992, followed by around 10 years in CSIRO and then WEHI. His research interests include HTS library design, medicinal chemistry hit-to-lead and lead optimization, and computer-aided peptidomimetic design in order to generate compounds with potential therapeutic utility and of value. He has over 26 separate and mostly licensed pharmaceutical patents and a number of compounds in various stages of development, from preclinical to one currently in phase I clinical trials for anxiolysis. He also consults widely for the Australian Biotechnology Industry. Close window Histone Acetyltransferase Inhibitors, from Screening to Optimization - a Tricky Track
Makonen Belema received a B.A. in Chemistry from Swarthmore College and a Ph.D. in Synthetic Organic Chemistry from Yale University under the mentorship of Professor F. E. Ziegler before joining Bristol-Myers Squibb in 1996. Early in his industrial career, he worked on a retinoid and an IKK project as part of a broader effort directed at the treatment of dermatological and immunological disorders, respectively. His work over the past decade has focused on the exploration of novel HCV and HIV mechanisms, the most noteworthy result of which include the discovery of the HCV NS5A replication inhibitor daclatasvir (DaklinzaTM).
Close window Direct and Synergistic Inhibition of The HCV NS5A Protein
Dr. Gonçalo Bernardes is a Group Leader at the Department of Chemistry, University of Cambridge, U.K.
He is also the Director of the Chemical Biology and Pharmaceutical Biotechnology Unit at the Instituto de Medicina Molecular, Portugal. After completing his D.Phil. degree in 2008 at the University of Oxford, U.K., he undertool postdoctoral work at the Max-Planck Institute of Colloids and Interfaces, Germany, and the ETH Zürich, Switzerland, and worked as a Group Leader at Alfama Lda in Portugal. He started his independent research career in 2013, and his research group interests focus on the development of site-selective chemical protein modification for basic biology and drug development. He is a Royal Society University Research Fellow and in 2015 he was awarded a Starting Grant from the European Research Council. In 2013, he was awarded the European Federation for Medicinal Chemistry (EFMC) Prize for Young Medicinal Chemist in Academia. Close window RSC Prize Lecture:
Paul obtained his PhD in from Imperial College working with Dr David Widdowson on the application of aromatic chromium tricarbonyl complexes to natural product synthesis in 1984 and in the same year joined Glaxo. He worked for the company for 25 years and worked in a number of therapeutic areas and target classes but with a main focus on Neuroscience and in particular pain, working on targets including enzymes (iNOS, COX2), GPCR targets (CB2 and adenosine a1 receptors) and ion channels (P2X7 and Cav2.2) in each case identifying compounds which reached clinical evaluation.
In 2008 Paul left GSK to join Almirall in Barcelona as Head of Medicinal Chemistry and whilst there continued his interest in ion channel drug discovery initiating a number of new ion channel focussed projects for both neuroscience and respiratory indications.
In 2013 he returned to the UK to take up his current position which is focussed on both establishing new external collaborations and managing internal neuroscience projects.
Close window The Painful Reality of Drug Discovery and Development
Maria Laura Bolognesi holds the position of Professor of Medicinal Chemistry at the Department of Pharmacy and Biotechnology at the University of Bologna.
She received her PhD in Pharmaceutical Sciences in 1996 and carried out postdoctoral work at the University of Minnesota, Minneapolis. She was awarded the positions of Special Visiting Researcher at the University of Brasilia in 2014, and Distinguished Visiting Professor at the Complutense University of Madrid in 2009. She currently serves as Associate Editor of the Journal of Medicinal Chemistry. Her current research explores the development of multitarget and theranostic small molecules against neurodegenerative and neglected tropical diseases. Close window Tackling Neurodegenerative Diseases Through Multi-Target and Theranostic Small Molecules
Martin Burke completed his undergraduate degree in chemistry at Johns Hopkins University in 1998, a Ph.D. in organic synthesis at Harvard University in 2003, and an M.D. at Harvard Medical School in 2005.
He is now a Professor in the Department of Chemistry at the University of Illinois at Urbana-Champaign. Marty’s research focuses on small molecules that replicate the functions of missing proteins, thereby operating as prostheses on the molecular scale. To enable such studies, Marty's group created a machine that builds molecules from pre-fabricated building blocks. This advance helps make the process of complex small molecule synthesis as simple, efficient, and flexible as possible. Close window Towards a More Generalized and Automated Approach for Small Molecule Synthesis
Dr. Michael Boettger works as an Early Clinical Leader in the Clinical Sciences Experimental Medicine Group at Bayer. The main focus lies on forwarding innovative preclinical assets to clinical proof of concept. Indication areas covered include ophthalmology and gynecology.
Dr. Boettger is a physician by training with board certification in physiology. Prior to his current assignment, he held clinical and preclinical positions in neurology, physiology and ophthalmology in Würzburg, Jena, Wuppertal and London. Close window Regorafenib Eye Drops for Wet AMD – Challenges in Translatability of Preclinical Data Into Clinical Efficacy
CURRENT TITLE AND POSITION: Associate Professor at Molecular Biotechnology and Health Sciences Dept, University of Torino, Italy.
RESEARCH FIELDS: Design, implementation and interpretation of simple and combined molecular descriptors in membrane-like environments. The impact of ionization on molecular properties. Molecular interactions governing drug permeability. QSAR/QSPR strategies applied to ADME topics and mechanistic interpretation of the resulting statistical models. Prediction and experimental determination of cyclodextrin/ligand complexes stability constants. EDUCATION AND FORMER PROFESSIONAL EXPERIENCE: B.Sc. in Pharmaceutical Chemistry and Technology in 1992 and B.Sc. in Pharmacy in 1994 (University of Torino, I.), Ph.D. in Pharmaceutical Sciences in 1997 under the supervision of prof. B. Testa at the University of Lausanne (CH). Close window The Need of Implementing Intramolecular Hydrogen Bonding (IMHB) Considerations in Drug Discovery and How to do it
Dr. Alessio Ciulli is currently an Associate Professor in Chemical & Structural Biology at the University of Dundee. After graduating Magna Cum Laude in Chemistry in 2002 from his hometown Florence under guidance of the late Professor Ivano Bertini, Alessio was awarded a Gates Scholarship to study at the University of Cambridge. His PhD (2006, Chemical Biology) focused on biophysical and structural studies of protein-ligand interactions under the supervision of Professor Chris Abell at the Department of Chemistry and Dr Glyn Williams at fragment-based drug discovery company Astex Pharmaceuticals. Following post-doctoral research with Professor Abell and Professor Sir Tom Blundell, he obtained a Human Frontier Science Program visiting Fellowship at Yale University to start collaboration with Professor Craig Crews, and then returned to Cambridge to start his independent research career upon the award of a BBSRC David Phillips Fellowship (2010). In 2013 Alessio was awarded an ERC Starting Grant and moved his laboratory to the School of Life Sciences at the University of Dundee as Principal Investigator within the Division of Biological Chemistry and Drug Discovery. He is the recipient of the MIUR Award ‘Messaggeri della Conoscenza’ with the University of Messina, Italy (2013), the ‘Talented Young Italians Award’ for Research and Innovation (2014), the European Federation for Medicinal Chemistry (EFMC) Prize for a Young Medicinal Chemist in Academia (2015) and the International Chemical Biology Society (ICBS) Young Chemical Biologist Award (2015).
Close window RSC Prize Lecture:
Dr Miles Congreve, Vice President of Chemistry at Heptares Therapeutics
Heptares is a clinical-stage company creating novel medicines targeting G protein-coupled receptors (GPCRs) using structure based drug design and/or fragment based drug discovery.
Miles obtained a BSc in biological chemistry from Leicester University and a PhD in synthetic chemistry from Cambridge University, before joining Glaxo in 1993. In 2001 he joined Astex Therapeutics working on fragment-based drug discovery. He joined Heptares in 2008. Miles is a faculty member of the Drew Residential School on Medicinal Chemistry and Biology in Drug Discovery (ResMed) where he teaches the principles of Fragment Based Drug Discovery. Miles is on the Editorial Advisory Boards of the Journal of Medicinal Chemistry and Current Topics in Medicinal Chemistry. In 2015 Miles was one of the awardees of the Royal Society of Chemistry’s Malcolm Campbell Memorial Prize for his part in the seminal contributions to GPCR drug discovery made by Heptares since 2007. Close window Identification of Allosteric Inhibitors of GPCRs Using SBDD
Benoit Déprez is a pharmacist and chemist by training. He did his PhD work under the supervision of Pr. André Tartar at the Institut Pasteur de Lille. After his PhD, he has managed parallel synthesis at Cerep (acquired by Eurofins) and later drug discovery operations at Devgen.
He is co-founder of Apteeus and consultant for Investments Funds and biotech companies. He is currently the founder and director of the Drug Discovery Lab at Inserm and Institut Pasteur de Lille (U761, now U1177, “Drugs & Molecules for Living Systems”). He is author of more than 90 publications in peer-reviewed international journals and 19 patents. He has a H-factor of 25 (i10 = 52, i50 = 12). As faculty member, he teaches the classes of Industrial Phamacy (management of pharma R&D, scientific bases of marketing and pharmaceutical affairs). He is corresponding member of the Academie Nationale de Pharmacie. Close window Pharmacological Reversion of Antibiotic Resistance in Mycobacterium Tuberculosis : Design of SMART Trojan Molecules to Reprogram The Bacteria
Dr. Eric Desarbre obtained his PhD in 1995 from University of Orléans (France) under the supervision of Pr. Jean-Yves Merour for the preparation of pyrrolo[2,3-b]pyridine derivatives (7-azaindoles). He then joined Pr. Jan Bergman’s department at the Karolinska Institute (Stockholm, Sweden) for a post-doctoral position where he prepared indolo[2,3-c]carbazole moieties. After 5 years at Pharmacia Corporation (Stockholm, Sweden), he joined in 2001 the research department of Basilea Pharmaceutica (Basel, Switzerland) where he is involved in antimicrobial projects. Since 2004, as responsible of the chemist team and deputy project leader for Gram-negative antibacterial projects, he is mainly working with -lactam scaffolds. His chemistry activities recently led to the discovery of monobactam antibiotic BAL30072.
Close window New Antibacterial Agents in the Pipeline
Alexander Dömling studied Chemistry & Biology at the Technical University Munich and performed his PhD with Ivar K. Ugi. Then he performed his postdoc in the laboratory of Nobel Laureate Barry Sharpless as a Feodor Lynen fellow of the Humboldt society. After several years as professor at the University of Pittsburgh he recently became chair and professor of the department of drug design at the University of Groningen. His scientific interest include basics and applications of multicomponent reaction chemistries (MCR). MCR allows for the rapid generation of unprecedented chemical diversity which is tested in the Dömling laboratory for difficult biological targets, such as protein protein interactions (p53-MDM2, PD1-PDL1 etc). He also developed the pharmacophore based web-based platform ANCHOR.QUERY allowing to desktop-screen billions of instant synthesizable MCR molecules. In the context of difficult protein protein interactions his laboratory is developing innovative rapid macrocycle syntheses. He is author of >200 papers and multiple patent applications.
Close window Expanding the Macrocycle Chemical Space
Gerhard Ecker is Professor of Pharmacoinformatics and Head of the Pharmacoinformatics Research Group at the Department of Pharmaceutical Chemistry, University of Vienna. He also coordinates the research focus “Computational Life Sciences” of the Faculty of Life Sciences.
Gerhard received his doctorate in natural sciences from the University of Vienna and performed his post-doctoral training at the group of J. Seydel in Borstel (Germany). His research focuses on computational drug design, with special emphasis on drug-transporter interaction and prediction of off-target effects. Besides this, he coordinates the Open PHACTS project, which aims at creating an Open Pharmacological Space by semantic integration of public databases. Gerhard is Editor of Molecular Informatics, served 2009 – 2011 as President of the European Federation for Medicinal Chemistry, and is currently Vice Dean at the Faculty of Life Sciences. Close window Exploiting Linked Open Data - Transporter Profiling and Beyond
Steve Elmore, Ph.D. Vice President Target Enabling Science and Technology Discovery Research AbbVie Dr. Elmore currently holds the position of Vice President in Discovery Research at AbbVie responsible for a core science and technology organization called Target Enabling Science & Technology focused on target discovery/validation and small molecule lead discovery and characterization. This multi-disciplinary group integrates chemical biology, proteomics, functional genomics, genetic/genomic profiling and cell-based phenotypic screening for target discovery/validation and traditional high throughput screening with fragment-based drug discovery for lead discovery. Prior to this role, Dr. Elmore has held multiple leadership and scientific positions at AbbVie/Abbott including VP of Early Discovery Research and Director in Oncology research responsible for apoptosis research. He and his teams have discovered and advanced numerous drug candidates to the clinic, including ABT-199 (venetoclax). An organic chemist by training, Steve earned a Bachelor of Science degree in Chemistry from Southern Illinois University at Carbondale and a Ph.D. in synthetic organic chemistry from The Ohio State University. Close window Releasing the Brake on Apoptosis. Discovery of Bcl-2 Family Protein Inhibitors
Patrick Eyers is Reader in Chemical Biology in the Department of Biochemistry at the University of Liverpool.
He received his PhD with Professor Sir Philip Cohen, where he ‘target-validated’ some of the first kinase inhibitors and co-discovered the 'gatekeeper' residue, a determinant for small molecule interaction that dictates sensitivity to many kinase ligands, including approved drugs. After postdoctoral work with Jim Maller, where he worked on fundamental aspects of the Xenopus cell cycle, he set up his lab with an independent MRC fellowship. His research currently centres on the exploitation of small molecule ‘tool’ compounds to investigate cell signalling. In particular, he employs chemical biology to evaluate protein (pseudo)kinases, whose wide variety of signalling modes driven through nucleotide and small molecule interactions are increasingly appreciated. More recently, he has established expertise in the analysis of non-kinase targets and kinase drug-resistance mechanisms through combined screening, repurposing and target-validation approaches. Close window New Pseudokinase Drug Targets in the Human Kinome
Daniel L. Flynn, PhD is currently Founder and Chief Scientific Officer of Deciphera Pharmaceuticals. Prior to Deciphera, Daniel joined Warner-Lambert/Parke Davis Pharmaceuticals (1983-1988). He then moved to Searle Pharmaceuticals as Section Head in Medicinal Chemistry (1988-1998). In 1998, Dan joined Amgen, Inc as Director of Medicinal Chemistry. In 2000, he moved to Cambridge, MA, as Senior Director of Chemistry with Millennium Pharmaceuticals. Daniel received his B.S. in pharmacy from the University of Kansas (1977), his PhD in medicinal chemistry from the University of Kansas (1981) under the mentorship of Professor Les Mitscher, and a post-doctorate in synthetic organic chemistry at Indiana University with Professor Paul Grieco (1983),
Close window Switch Control Inhibitors: an Advance in Type II Kinase Inhibition
Fabrizio Giordanetto graduated with first class honors in Medicinal Chemistry in 2000 from University of Genoa (Italy). He completed his Ph.D. in Computational Medicinal Chemistry in 2003 at University of London (UK) while working for the chemistry unit of Pharmacia (Pfizer) in Nerviano, Italy. Following positions at AstraZeneca (Sweden) as Principal Scientist and Preclinical Project Leader and at Taros Gmbh (Germany) as Head of Medicinal Chemistry, he has recently joined DE Shaw Research LLC (New York) where he leads medicinal chemistry activities and drug discovery projects. During his career, he worked on several drug discovery programs resulting in multiple clinical candidates spanning oncology, CNS and cardiovascular indications and >90 peer–reviewed publications, book chapters, and international patents.
Close window Intramolecular Hydrogen Bond Expectations in Medicinal Chemistry
Dr. Cristiano R. W. Guimarães received his Ph.D. in Theoretical/Organic Chemistry from the Federal University of Rio de Janeiro in 2001, followed by a postdoctorate with Prof. William Jorgensen at Yale University.
In 2005, Dr. Guimarães joined Amgen, where he worked as a Scientist for two years. He then moved to Pfizer, where he worked until early 2014 as a Senior Principal Scientist. The main focus of his research activities as a Scientist was the development and application of computational methodologies in drug design, having resulted in over 50 scientific articles and patents. He is currently the Director of Radical Innovation at Aché Laboratórios Farmacêuticos, one of top pharmaceutical companies in Brazil. Close window Research, Development & Innovation at Aché Laboratórios Farmacêuticos
Wolfgang Haap joined Roche in Basel, Switzerland in 2001. He is working as a project team leader and expert scientist in medicinal chemistry in the field of lead identification and optimization up to clinical candidate selection. Before starting at Roche he spent from 1998 on three years at Ciba in Grenzach, Germany (now BASF) in the research area of the discovery of new antibacterials.
Close window Discovery and Development of the Highly Potent, Highly Selective Cathepsin S Inhibitor RG7625 for the Treatment of Autoimmune Diseases
Christian Heinis studied biochemistry at the Swiss Federal Institute of Technology in Zurich (ETH). After a PhD in the research group of Prof. Dr. Dario Neri at ETH, he did two post-docs, the first one with Prof. Dr. Kai Johnsson at the Ecole Polytechnique Fédérale de Lausanne (EPFL) and the second one with Sir Gregory Winter at the Laboratory of Molecular Biology (LMB) in Cambridge, UK. In 2008 he started as Assistant Professor at EPFL (supported with an SNSF professorship) and was promoted in 2015 to Associate Professor. The main research interest of Christian Heinis is the development of peptide macrocycle therapeutics. Christian is a scientific co-founder of the start-up company Bicycle Therapeutics.
Close window Phage-Encoded Combinatorial Chemical Libraries Based on Bicyclic Peptides
David Hepworth is Senior Director of Medicinal Chemistry at Pfizer based in the Cambridge, MA site. Currently he works in support of the Inflammation and Immunology Research Unit, but has previously worked in a number of disease areas in Pfizer, including metabolic and cardiovascular diseases, and at a number of sites including Sandwich, UK and Groton CT. David has a particular interest in the potential of Solute Carrier (SLC) proteins as drug targets.
Close window The Design and Evaluation of URAT1 Inhibitors for the Treatment of Hyperuricemia and Gout
Joerg is a trained Organic and Medicinal Chemist and acquired his Ph.D. in Germany on the synthesis of alkaloids as antimalarial agents. He started his professional career in 1998 as Medicinal Chemist at Grunenthal Pharmaceuticals in Germany, delivering the marketed analgesic Tapentadol.
From 2003 to 2006, he headed the Medicinal Chemistry Department of Barcelona-based Laboratorios Esteve. In 2006, Joerg joined AstraZeneca’s CNS/Pain Unit in Soedertaelje, Sweden, as Project Leader, and later headed the Neuroscience Lead Generation. In 2012, Joerg was selected to join the newly formed ‘virtual’ Neuroscience Unit in Boston as Director for Discovery and Preclinical Sciences, and in this role is responsible for pioneering a novel concept of driving Research and Development via increased use of academic and industry collaborative networks. In his career, Joerg worked predominantly in the Pain and Neuroscience disease areas, where he delivered marketed drugs as well as several clinical candidates. Joerg has edited, authored or contributed to more than 45 publications, 50 patent applications and several books and book chapters. Close window Discovery of AZD3241 is a Potent and Selective Myeloperoxidase Inhibitor for the Treatment of Neurodegenerative Disorders
Dr Howard is a Founding Scientist and Chief Scientific Officer at Spirogen. He has been conducting research into the pyrrolobenzodiazepine (PBD) family of antitumor antibiotics for twenty years in both academia and industry. Philip has worked as a part of a multi-disciplinary team, supported by Cancer Research UK and Spirogen, on the synthesis, biological evaluation and development of the PBD dimer SG2000 (Auven), which is currently in Phase II clinical trials. Since 2008 he has been working on the development of the PBDs as payloads for antibody drug conjugate therapy with a number of companies including Spirogen, MedImmune, Genentech and Seattle Genetics. His work at MedImmune is focused on the development of their PBD ADC platform. At the time of writing, several PBD based antibody drug conjugates, arising from Spirogen collaborations, are the subject of Phase I clinical trials.
Close window The Development of Pyrrolobenzodiazepine in Antibody Drug Conjugates
Bob Jacobs is Vice President of Chemistry at Anacor Pharmaceuticals, with responsibility for the discovery and application of novel boron-containing drug molecules to anti-parasitic, anti-microbial, anti-fungal and anti-inflammatory diseases. Prior to joining Anacor in 2013, Dr. Jacobs was Director of Chemistry at SCYNEXIS, Inc., where he led the human African trypanosomiasis drug discovery programme in collaboration with Anacor and DNDi that delivered SCYX-7158 to clinical trials for this disease. Dr. Jacobs’ professional career began as a medicinal chemist with AstraZeneca Pharmaceuticals (and predecessor companies) in the US and UK, where he contributed over a 17 year career to medicinal chemistry and process development projects in the pulmonary, CNS and oncology therapeutic areas. Dr. Jacobs received his Ph.D. in Organic Chemistry from Cornell University in 1985, and was a post-doctoral research associate at the University of Illinois, Urbana-Champaign from 1985-87.
Close window Utilization of Novel Benzoxaboroles as Drug Candidates to Treat Neglected Tropical Diseases
Johanna (Hanneke) Jansen, Ph.D.
Head Computer-Aided Drug Discovery – Emeryville
Novartis Institutes for BioMedical Research
Hanneke Jansen is Head of the Computer-Aided Drug Discovery (CADD) group at the Emeryville site of the Novartis Institutes for BioMedical Research. Prior to Novartis, Hanneke worked at Chiron Corporation and at Astra. Her group at Novartis supports drug discovery for the local and global organization by developing and applying CADD approaches to projects at all stages of the portfolio. Her research interests include the design of relevant compound sets for hit generation, improved predictive modeling that leverages large complex datasets, and developing computational chemistry & data-mining methods that can be integrated into state-of-the-art workflows to inform decision-making from target-ID and validation through hit generation and optimization. Hanneke is a Fellow of the American Chemical Society. She received her Ph.D. in computational medicinal chemistry from the School of Pharmacy, University of Groningen (Netherlands) and completed a postdoctoral term at the BioMedical Center of Uppsala University (Sweden). Close window Inhibition of Prenylated KRAS: Tools to Discover and Characterize RAS Ligands
Neil W Johnson, Ph.D.. US Chemistry Talent Development Lead for GSK.
Bachelor’s degree in chemistry from Fort Lewis College in 1988 followed by PhD at Johns Hopkins University in 1994. 5 years at Cephalon Inc., a small bio-tech interested in the discovery of neuro-protective agents, now part of Teva. Joined SmithKine Beecham in 1999 which soon after became GSK. He originally joined the Oncology group and for most of his time at GSK worked in the area of kinase inhibition, leading numerous programs clinical candidates. In 2008 GSK reorganized to performance units where he became a member of the Cancer Epigenetics DPU. He has been a member of multiple programs related to Cancer Epigenetics research and recently led the LSD1 inhibitor program which resulted in the selection of a clinical candidate. Close window The Identification of GSK2879552, a Mechanism Based Irreversible Inhibitor of the Histone Lysine Demethylase LSD1
Eric H. Karran PhD is a molecular biochemist by training. He is currently at AbbVie where he is Vice President and Site Head of the Foundational Neuroscience Center in Cambridge, Boston. Previously Eric was the Director of Research for Alzheimer’s Research UK.
He has held senior positions in a number of companies, including SmithKline Beecham (now GSK), Pfizer, Eli Lilly and at Johnson and Johnson. Eric has specialized in Neuroscience research, particularly Alzheimer’s disease and cognitive impairment, for the past 20 years. Eric is a Visiting Professor in the Department for Human Genetics at the Catholic University of Leuven, Belgium; an Honorary Senior Research Associate in the Department of Molecular Neuroscience at the Institute of Neurology, University College London; and Visiting Professor of Neurodegenerative Diseases at the University of Lincoln, United Kingdom. Close window Possibilities and Pitfalls: Disease Modifying Drugs for Alzheimer's Disease
Douglas Kell is Research Chair in Bioanalytical Science in the School of Chemistry/Manchester Institute of Biotechnology at The University of Manchester (2002-present).
Douglas’ interests are focused on the development and application of novel analytical methods to the solution of complex biological problems. The approach, using experimental and computational methods, is typically referred to as Systems Biology. He was Top Scholar, Bradfield College; at Oxford University he read Biochemistry, gained a Distinction in Chemical Pharmacology, obtained a DPhil there, and was a Senior Scholar of St John’s College. Douglas held numerous positions at the University College of Wales, Aberystwyth, was Founding Director, Aber Instruments Ltd, held a Personal Chair at the University of Wales, and was Director of Research at its Institute of Biological Sciences. From 2005-2008 Douglas was Director, BBSRC Manchester Centre for Integrative Systems Biology and from 2008-2013 was seconded 0.8 FTE as BBSRC Chief Executive. Close window The Cellular Uptake of Pharmaceutical Drugs is Transporter-Mediated - A Problem not of Biophysics but of Systems Biology
Prof. Dr. Horst Kessler, Carl von Linde Professor, Senior Fellow at the Institute for Advanced Study, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany
Current research field: Medicinal Chemistry. Design and synthesis of peptides and peptidomimetics and their functionalization. Elucidation functions of integrin subtypes using novel highly superactive and selective ligands and their use in medicine (for molecular imaging, for coating of biomaterials and as drug candidates) and for biophysical studies.
Study chemistry in Leipzig and Tübingen (1958-1963). 1966 Ph.D. in Tübingen. 1971-89 Full Professor in Organic Chemisty in Frankfurt., 1989- 2008 Professor of Organic Chemistry and Biochemistry TU München (TUM). Since 2008 Emeritus of Excellence TUM and appointment as Carl von Linde Professor at the Institute for Advanced Study, TUM.
Close window Peptides and Peptidomimetics: Overcoming Problems of Activity, Selectivity and Bioavailability of Integrin Ligands
Dr Ross King
Professor of Machine Intelligence
Research field: Artificial Intelligence/chemoinformatics Education and former professional experience: PhD Computer Science, Turing Institute MSc Computer Science, University of Newcastle upon Tyne BSc Microbiology, University of Aberdeen. Close window Robot Scientists, the Replication Crisis, and Cancer
Prof Stefan Knapp studied Chemistry at the University of Marburg (Germany) and at the University of Illinois (USA). He did his PhD in protein crystallography at the Karolinska Institute in Stockholm (Sweden) (1996) and continued his career at the Karolinska Institute as a postdoctoral scientist (1996-1999).
In 1999, he joined the Pharmacia Corporation as a principal research scientist in structural biology and biophysics. He left the company in 2004 to set up a research group at the Structural Genomics Consortium at Oxford University (SGC). From 2008 to 2015 he was a Professor of Structural Biology at the Nuffield Department of Clinical Medicine (NDM) at Oxford University (UK) and between 2012 and 2015 he was the Director for Chemical Biology at the Target Discovery Institute (TDI). He joined Frankfurt University (Germany) in 2015 as a Professor of Pharmaceutical Chemistry. He still remains associated to the SGC as a visiting Professor at Oxford University where he still run a research group. His research interests are the rational design of selective inhibitors that target protein kinases as well as protein interactions modules that function as reader domains of the epigenetic code. Close window Validating New Epigenetic Targets by Selective Protein Interaction Inhibitors of Bromodomains
Dr. Joseph A. Kozlowski completed a PH.D from the University of California, Santa Barbara, followed by an N.IH. post-doctoral fellowship at Princeton University. He joined Schering Plough in 1987 and is currently working at Merck & Co. in Rahway New Jersey.
Joe is a Senior Principal Scientist, working in the Infectious Diseases area. His work at Merck has included all phases of drug discovery, from early lead identification through involvement in clinical development teams. Additionally, Joe has worked in many areas of Medicinal Chemistry and has placed multiple compounds into clinical development. Close window Discovery of the HCV NS5A Inhibitor MK-8408 (RUZASVIR)
Bernd Kuhn earned his Ph.D. in Physical Chemistry at the Swiss Federal Institute of Technology, Lausanne, Switzerland, and then completed postdoctoral research as a DAAD fellow in macromolecular simulations with Prof. P. Kollman at the University of California, San Francisco.
In 2000 he joined the start-up company Prospect Genomics and one year later moved to the Computer-aided Drug Design group at F. Hoffmann-La Roche, Basel, Switzerland. He is currently a Senior Principal Scientist with a focus on new structure-based computational methods and their application to drug design projects. He has contributed to six compounds in clinical development and coauthored more than 130 scientific articles and patents. Close window Intramolecular Hydrogen Bonding as a Design Element in Medicinal Chemistry
Dr. Jin Li
Chairman and CEO, HitGen
Dr Li holds 28 years biopharmaceutical experience (at Protherics and AstraZeneca), with senior scientific and leadership roles in early stage research; as well as experience in initiating and leading major collaboration, research and outsourcing programmes. Before founding HitGen, he held Global Director positions of Compound Sciences and Computational Sciences at AstraZeneca. This included responsibility for computational chemistry, computational biology and compound collection enhancement. Dr Li completed his BSc at Sichuan University, and PhD in macromolecular sciences at Aston University. He then completed post-doctoral research in theoretical biochemistry at Manchester University, UK. Dr Li is also a Fellow of the Royal Society of Chemistry, the Guest Professor of Sichuan University and the Expert with Outstanding Contribution to Sichuan Province. He and his team have gained lots of rewards from different levels. Close window DNA-Encoded Chemical Library for Protein-Protein Interactions
John is Director of Medicinal Chemistry and Project Leader within Discovery Partnerships with Academia (DPAc) at GlaxoSmithKline.
His role in DPAc involves leading drug discovery projects in partnership with world-leading academic researchers in Europe in parallel to identifying and evaluating further opportunities for integrated collaborations. John has over seventeen years experience within the pharmaceutical industry and has led numerous drug discovery projects, across various target classes and therapeutic areas, delivering multiple clinical candidates. He trained as a synthetic organic chemist, gaining a PhD at The University of Manchester, and joined SmithKline Beecham as a medicinal chemist in 1999. Close window First Time Disclosure of a Development Candidate to Treat Severe Acute Pancreatitis through a Drug Discovery Partnership Between GSK and the University of Edinburgh
Dr. Philip S. Low is the Director of the Purdue University Center for Drug Discovery and the Ralph C. Corley Distinguished Professor of Chemistry.
Dr. Low has spent over 39 years exploring novel methods for drug targeting, and characterizing the structure, function, and pathologies of the erythrocyte membrane. He has published >350 scientific articles and has >50 US patents/patents pending. Eight drugs stemming from his research are undergoing human clinical trials and three companies (Endocyte Inc., OnTarget Laboratories Inc., and HuLow LLC) have been founded to commercialize his discoveries. Dr. Low has received an NIH MERIT Award, the ACS Award for Cancer Research (Sosnovsky Award), the AACR Award for Outstanding Chemistry in Cancer Research, both of Purdue's awards for outstanding research (McCoy and Sigma Xi Awards), the University’s highest career achievement award (Morrill Award), and numerous other National and International awards. Dr. Low received his B.S. in Chemistry from Brigham Young University (1971) and his Ph.D. in Biochemistry from UCSD (1975). Close window Ligand-Targeted Therapeutic and Imaging Agents for Multiple Human Diseases
Antonio Macchiarulo is Associate Professor of Medicinal Chemistry at the Department of Pharmaceutical Sciences of the University of Perugia (Italy).
He received his PhD in Chemistry and Technology of Drugs in 2004, and was then awarded with a Marie Curie postdoctoral fellowship at the European Bioinformatics Institute in Cambridge (UK), where he worked on selectivity and competition of substrate recognition by enzymes. Antonio Macchiarulo is actually member of the Scientific Committee of the European School of Medicinal Chemistry (ESMEC, users2.unimi.it/ESMEC). In collaboration with Prof. Ursula Grohmann, he has recently been awarded with an ERC Ideas Advanced Grant for a research project aimed at the development of novel therapeutic agents targeting Indoleamine 2,3-dioxygenase (IDO) in autoimmunity and neoplasia (ERC-2013-AdG 338954-DIDO). Close window Targeting the Janus-Faced Nature of IDO1 in Immuno-Oncology
Dr. MISLIN Gaëtan (Lucien Alfred), PhD, 44 years old, French citizen
Chargé de Recherches (Research Officer) at Centre National de la Recherche Scientifique (CNRS). Current position : Team « Bacterial Membrane Transport », Laboratory of Biotechnology and Cell Signaling, School of Biotechnological Engineering (ESBS), University of Strasbourg. Research interests : Chemistry of bacterial siderophores : Isolation and characterization. Bacterial siderophores and their synthetic analogues are our sources of inspiration in the design of innovative therapeutic strategies (antibiotics, chelating agents, etc.). Education : PhD in 1998 (University of Strasbourg, France, Dir.: Dr. Michel FRANK-NEUMANN, ). 1999-2001: Postdoctoral Fellow (Catholic University of Louvain, Belgium, Dir: Pr. Léon GHOSEZ). Hired by CNRS: 2001. PI since 2006. Close window Enterobactin-Dependent Iron Uptake Pathway as a Gate for Antibiotic Trojan Horse Strategies Against Pseudomonas Aeruginosa
Muneto Mogi has more than 20 years of global pharmaceutical R&D experience across various indications such as autoimmunity, respiratory, CNS, urology, infectious diseases, cardiovascular, and ophthalmology.
Muneto obtained his BA in chemistry from Boston University and his PhD in pharmaceutical science from Kyoto Pharmaceutical University. His career as a drug hunter began at Bayer in Kyoto, Japan. He joined Novartis Institutes for Biomedical Research in 2005 and he is currently director of global discovery chemistry and head of ophthalmology chemistry located in Cambridge, Massachusetts. Close window The Back of The Eye: Treatment Challenges and Opportunities
Carlos A. Montanari. Associate Professor at Institute of Chemistry of Sao Carlos, University of Sao Paulo (USP). Ph.D. in Organic Chemistry (1991) from USP.
Two decades of expertise in data mining in the discovery of bioactive chemicals, focusing on small molecules and use of methods for chemistry, with wide application in in silico-based screening on biomacromolecule targets and ligands (TBVS and LBVS). Eight years of conceptual development for the exploration of chemical-biological space of trypanocidal agents, including drug-and-binding properties similar to virtual screening and chemical synthesis: virtual screening, expression-isolation-purification of proteins, molecular docking, structure-activity and structure-property (SAR/SPR) relationships, synthesis of bioactive new trypanocidals, biocalorimetry for determining enzymatic mechanism of action and thermodynamic signature. Close window Molecular Design, Synthesis and Trypanocidal Activity of Dipeptidyl Nitriles as Cruzain Inhibitors
Prof. Dr. Christa E. Müller Head of Pharmaceutical Chemistry I, Pharmaceutical Institute http://mueller-group.pharma.uni-bonn.de Research field: Medicinal chemistry of purine-binding membrane proteins (P2, adenosine, adenine receptors, and ecto-nucleotidases); lipid-activated GPCRs, orphan GPCRs 1988 Ph.D. (Dr. rer. nat.), University of Tübingen 1989/90 and 1992 Postdoctoral scientist at NIH, Bethesda, Maryland, USA 1994-1998 Associate Professor (C3) University of Würzburg since 1998 Full Professor (C4) University of Bonn, Germany 2001-2004 and 2010-2015 Vice-rector at the University of Bonn Close window Medicinal Chemistry of Purinergic Signalling: Targets and Drugs for the Immunotherapy of Cancer
Cristina Nevado was born in Madrid in 1977. She studied Chemistry at the Autónoma University of Madrid and graduated in 2000.
In October 2004 she received her PhD in Organic Chemisty at the same university working with Prof. Antonio M. Echavarren in the cyclization of 1,6-enynes catalyzed by late transition metals. In December 2006 she joined the lab of Prof. Alois Fürstner as a post-doc at the Max-Planck-Institut für Kohlenforschung (Germany) where she was part of the team who conquered the first total synthesis of Iejimalide B. In May 2007 she joined the Organic Chemistry Institute of the University of Zurich as an Assistant Professor. In February 2013 she was promoted to Full Professor. Close window Potent and Highly Selective Bromodomain Ligands… a Platform for Reaction Discovery
Ronan has been leading the Oncology Discovery effort at Merck for the past 3 years, with a particular emphasis on small molecule approaches to enabling and enhancing immune-modulatory therapies in cancer. Prior to this he led Target Identification and Validation for Merck Oncology and built an early discovery pipeline including a mixture of biologics and small molecule programs. Ronan also spent 10 years in biotech, working on early target discovery, small molecules and biologics drug discovery and translational research. During this time he helped bring 3 programs into the clinic. Ronan did his post-doctoral work at the Dana Farber Cancer Institute with Dr. Ron DePinho, working on mouse models of cancer.
Close window Small Molecule Approaches to Immune-Modulation in Cancer
Krzysztof Palczewski, Ph.D., was named John H. Hord Professor and Chair of the Department of Pharmacology at Case Western Reserve University School of Medicine in Cleveland on September 1, 2005. Dr. Palczewski and his lab team have made several key scientific discoveries toward the understanding of phototransduction, the visual cycle, and the etiology of human blinding retinopathies. He also has served on a variety of national scientific advisory committees and the editorial boards of several well-known scientific journals. Two of his invented drugs are currently undergoing clinical trials. His contributions to vertebrate vision research include solving the structure of the light sensitive G protein-coupled receptor rhodopsin identifying novel elements such as miRNAs and non-coding RNAs; characterizing critical visual cycle proteins; applying novel imaging and functional assays to the retina, identifying blinding genetic mutations and devising pharmacological therapies for treatment of retinal dysfunction/disease.
Close window Molecular Pharmacodynamics of Visual Cycle Modulators in Protection Against Retinal Degeneration
Dr. Zhengying Pan received his bachelor degree in chemistry from Peking University in 1994, and obtained his Ph.D. in organic chemistry from Columbia University in 2000.
After a two-year postdoctoral training at Stanford University, he worked at several biotech companies in the United States including Celera Genomics, where he designed and synthesized a molecule now called “ibrutinib”, a drug for treating multiple B cell related malignancies. Since 2009, he returned to Peking University and continued working in the areas of medicinal chemistry and chemical biology. Currently he is distinguished research fellow at Peking University Shenzhen Graduate School. Close window Targeted Covalent Inhibitors of Bruton's Tyrosine Kinases - Design, Evaluation and Follow-up
Janeta Popovici-Muller is currently Director of Medicinal Chemistry at Agios Pharmaceuticals, leading small molecule programs to deliver drug candidates in the areas of cancer and rare genetic disorders of metabolism.
Before joining Agios in 2010, Janeta worked for 10 years at NeoGenesis Pharmaceuticals that later became Schering-Plough, and was acquired by Merck in 2009. During her tenure there, she contributed to several lead optimization programs in the fields of virology, inflammation and exploratory oncology. Janeta earned a PhD degree from Dartmouth College and has co-authored more than 50 publications in peer-reviewed journals, patents, invited lectures and presentations. Close window Discovery of AG-120 – A First-in-class Inhibitor of IDH1 Mutant Enzymes for the Treatment of Cancers Harboring IDH1 Mutations
E. Scott Priestley is currently a Senior Principal Scientist in the Cardiovascular Chemistry group at Bristol-Myers Squibb. He leads several ongoing cardiovascular drug discovery projects. His research interests include thrombosis and heart failure therapies, antivirals, G-protein coupled receptor modulators, serine protease inhibitors, and oligonucleotide therapeutics.
Scott received his BS in 1991 from Texas A & M University and his PhD in 1996 from the California Institute of Technology, where he worked with Professor Peter Dervan on non-natural nucleosides in DNA triple helix formation. He then moved to Scripps Research Institute and carried out post-doctoral research with Professor Chi-Huey Wong on aminoglycoside-RNA interactions. He joined DuPont-Merck Pharmaceuticals in 1998, and moved to Bristol-Myers Squibb in 2001 when it acquired DuPont Pharmaceuticals. Close window Discovery of a First-in-Class PAR4 Antagonist as a Novel Antithrombotic
Marc Robillard is founder and CEO of Tagworks Pharmaceuticals, a spin-out of Philips. Tagworks develops and applies bioorthogonal conjugation and elimination chemistry in living systems to improve the efficacy of cancer therapies and to enable novel approaches in companion diagnostics. Prior to spinning out in 2011 he worked at Philips Research on molecular imaging and drug delivery and at Kreatech Diagnostics on microarray detection. Marc obtained his MSc and PhD in bio(in)organic chemistry at, respectively, the University of Groningen and the Leiden Institute of Chemistry, The Netherlands.
Close window Antibody Imaging and Therapy Using in Vivo Click and Click-to-Release Strategies
Dr. Carsten Schmeck , Principal Scientist
BAYER Pharma AG, Drug Discovery, Medicinal Chemistry Wuppertal
Carsten joined BAYER in 1994, working on projects in the fields of atherosclerosis and lipid disorders, peripheral vascular disease, heart failure and since 2014 in kidney diseases. From 1994 to 2014 he had the opportunity to be part of several lead optimization projects (many times as team leader) which successfully discovered clinical candidates. Since 2014 he is working on earlier projects which are in their “hit to lead phase” in the field of kidney disease. Carsten studied chemistry in Göttingen in Germany, receiving his diploma from Prof. Dr. U. Schöllkopf in 1988. He got his Ph.D in 1991 from Prof. Dr. U. Groth working on an asymmetric synthesis of non-proteinogenic amino acids and dipeptides. From 1992 to 1994 he joined the group of Prof. Dr. L.S. Hegedus in Fort Collins, Colorado working chiral amino chromium carbene complexes and their use in the synthesis of amino acids. Close window Discovery of Clinical Candidate Ribuvaptan, a Dual Acting Vasopressin V1a/V2 Receptor Antagonist for the Treatment of Heart Failure
Gisbert Schneider has been Full Professor of Computer-Assisted Drug Design in the Department of Chemistry and Applied Biosciences at ETH Zurich since 2010. He received a doctorate in biochemistry from the Freie Universität Berlin in 1994. Prior to joining ETH, he worked in industrial research at Roche Pharmaceuticals, Basel (Head of Cheminformatics), and held the position of a full professor at the Goethe University in Frankfurt (Beilstein Endowed Chair for Chem- and Bioinformatics). Gisbert Schneider’s research activities focus on the development of innovative methods for virtual screening, molecular de novo design and adaptive autonomous systems in drug research. He is a co-founder of inSili.com LLC, Zurich, and AlloCyte Pharmaceuticals Ltd, Basel.
Close window Big Dada in Medicinal Chemistry?
Chris Schofield studied for a first degree in chemistry at the University of Manchester (1979-1982).
In 1982 he moved to Oxford to study for a DPhil with Professor Jack Baldwin on the synthesis and biosynthesis of antibiotics. In 1985 he became a Departmental Demonstrator in the Dyson Perrins Laboratory, Oxford University followed by his appointment as Lecturer in Chemistry and Fellow of Hertford College in 1990. In 1998 he became Professor of Chemistry, and in 2011 was appointed Head of Organic Chemistry. He is a Fellow of the Royal Society of Chemistry and of the Royal Society. His research group works at the interface of chemistry, biology and medicine. His work has opened up new fields in antibiotic research, oxygen sensing and gene regulation. Close window Mechanistic and Inhibition Studies on Metallo-Beta-Lactamases
Giulio Superti-Furga, PhD. is Scientific Director and CEO of the Research Center for Molecular Medicine of the Austrian Academy of Sciences in Vienna (CeMM), Austria and a Professor of Medical Systems Biology at the Medical University of Vienna.
He performed studies in molecular biology at the University Zurich, Genentech, and IMP/Vienna. He has a post-doctoral fellow and Team Leader at EMBL. He co-founded the biotech companies Cellzome and Haplogen. His expertise is systems pharmacology Close window Solute Carriers, Metabolism and Drug Response: a Magic Triangle
Dr. Masahiko Terakado
Medicinal Chemist with 20+ years experience. ONO Pharmaceutical Co., Ltd. Osaka Japan Medicinal chemistry (GPCR, Bioactive Lipid) 1994: PhD., Organic Chemistry, Tokyo Institute of Technology, Tokyo, Japan Close window Discovery of Novel LPA1 Antagonist: Design and SAR Studies
Peter Timmerman, PhD. Chief Scientific Officer (CSO) at Pepscan Therapeutics
Peter Timmerman studied Organic and Analytical Chemistry at the ‘Vrije Universiteit’ of Amsterdam (1984-1989). He obtained a PhD-degree in Supramolecular Chemistry (summa cum laude) from the University of Twente with David N. Reinhoudt (1994), where he was an Assistant Professor from 1995-2001. Thereafter, he joined to startup company Pepscan Therapeutics in Lelystad/NL, where he currently holds the position of CSO and as such drives further advances in protein mimicry technology for therapeutic antibody development and peptide businesses. He is the inventor of Pepscan’s proprietary and broadly applicable ‘2-CLIPS’ technology for conformationally constrained peptides. The technology is a.o. applied to the mapping of conformational and discontinuous antibody binding sites. Lately, the startup company Bicycle Therapeutics was granted a license to the CLIPS-technology for development of therapeutic 2-CLIPS peptides. Timmerman also led the development of a therapeutic peptide-based anti-VEGF-vaccine that is currently in Phase-IIa clinical testing. Since March 2007 he holds a Special Chair in ‘Protein Mimetic Chemistry’ at the Faculty of Science of the University of Amsterdam. Timmerman is co-author of >80 peer-reviewed scientific papers and >10 patents. Close window Discovery & Optimzation of Clips-Constrained Bicyclic Peptides (2clips) Using Pepscan Peptide Arrays
Mariola Tortosa obtained her B.S. in Chemistry from the Universidad Autónoma de Madrid (UAM) in 1999.
She then joined the group of Dr. R. Fernández de la Pradilla at the Instituto de Química Orgánica General (CSIC, Madrid, Spain) to carry out her graduate work on the development of new asymmetric methods using chiral sulfoxides. In 2005, she moved to The Scripps Research Institute in Florida (USA) to work as a Postdoctoral Fellow with Prof. William Roush. Her research in Florida was directed toward completion of the total synthesis of the antitumor agent Superstolide A using a transannular Diels–Alder strategy. In 2008 she returned to the Instituto de Química Orgánica General (Madrid, Spain) as a Juan de la Cierva fellow. In 2011 she started her independent research at the Universidad Autónoma de Madrid with a Ramón y Cajal contract. Her research interests include boron chemistry, asymmetric catalysis and the synthesis of natural products. Close window Nucleophilic Boron for the Preparation of Highly Functionalized Small Rings
Trond Ulven is professor of pharmaceutical chemistry with special assignments in entrepreneurship at the University of Southern Denmark.
He obtained his PhD in organic chemistry in from the Norwegian University of Science and Technology in 1999. Thereafter he stayed as postdoc at the Scripps Research Institute before moving moved to Denmark to the startup company 7TM Pharma in 2001 and further to the University of Southern Denmark in 2005. His research interests include drug discovery and medicinal chemistry with special focus on 7-transmembrane receptors, inflammation and metabolic diseases, as well as development of synthetic methods aimed at drug discovery. Close window Targeting Long-Chain Fatty Acid Receptors FFA1 and FFA4 for Treatment of Metabolic Diseases
Herman van Vlijmen graduated with a Master’s degree in Bio-Pharmaceutical Sciences at Leiden University and a PhD degree in Physical Chemistry at Harvard University
He worked 9 years at Biogen in the Boston area, ultimately as Senior Scientist, in the computational design of small molecule drugs and protein therapeutics. In 2005 he joined Tibotec, a Janssen company, as Director of Computational Drug Design. He is now Head of Computational Chemistry in the Discovery Sciences organization at Janssen, Pharmaceutical companies of Johnson & Johnson, located in Belgium. Since 2008 he is also Adjunct Professor of Computational Drug Discovery at Leiden University. Herman has more than 50 publications and is inventor on 8 patents. Close window Broad Multiparametric Profiling of Kinase Inhibitors
Tom von Geldern has been an independent consultant to the pharmaceutical and biotech industries since 2007, specializing in medicinal chemistry and discovery strategy and tactics, and with a particular focus on the development of treatments for neglected tropical diseases. Prior to this, Dr. von Geldern spent over 20 years in the pharmaceutical industry, most recently serving as a Research Fellow and Senior Group Leader at Abbott Laboratories. In this capacity he led medicinal chemistry efforts resulting in the identification of clinical candidates in the areas of oncology, inflammation, cardiovascular and metabolic diseases. He is an author of 84 peer-reviewed articles, an inventor on 52 US patent applications, and has lectured by invitation on more than 65 occasions.
Dr. von Geldern received S.B. degrees in Chemistry, Mathematics, and Biology from MIT, a Ph.D. in Chemistry from the University of California at Berkeley, and performed post-doctoral research at Stanford University. Close window The Discovery and Development of Novel Macrofilaricidal Agents for the Treatment of Onchocerciasis and Lymphatic Filariasis
Prof. Dr. Dr. h. c. Herbert Waldmann
11 June 1957 born in Neuwied, Rhein
1976-1985: Studied chemistry at the University of Mainz. Received a Ph.D. in Organic Chemistry in 1985 under the guidance of Prof. H. Kunz. 1985-1986: Postdoctoral fellow with Prof. George Whitesides at Harvard University, Cambridge, Massachusetts. 1986-1991: Habilitation at the University of Mainz. Obtained tenure in 1991. 1991: Appointment as Professor of Organic Chemistry at the University of Bonn. 1993: Appointment as Full Professor of Organic Chemistry at the University of Karlsruhe. 1999: Appointment as Director at the Max-Planck-Institute of Molecular Physiology Dortmund, Department of Chemical Biology and as Full Professor of Organic Chemistry at the University of Dortmund. 2005 to date: Head of the Chemical Genomics Center of the Max Planck Gesellschaft 2007-2008: Managing Director of the Center of Advanced European Studies and Research (“caesar”), Bonn 2014:Honorary Doctorate (Dr. h. c.) bestowed by Leiden University, NL Honours and Awards 1982: Adolf-Todt-Award. 1986:Friedrich Weygand Award for the Advancement of Peptide Chemistry. Award of the Johannes-Gutenberg-University of Mainz. 1991:Habilitanden-Preis of the ADUC. 1992: Carl Duisberg Award of the Gesellschaft Deutscher Chemiker. Dozenten-Price of the Fonds der Chemischen Industrie. 1997: Steinhofer Award of the Steinhofer Foundation, University of Freiburg. 2001: Otto-Bayer-Award. 2003:Max-Bergmann Medal 2004:F. C. Donders Professorship, Utrecht, Netherlands 2004:President of the Bürgenstock Conference 2004: Member of „Deutsche Akademie der Naturforscher Leopoldina, Halle/Saale“ 2005: Fellow of the Royal Society of Chemistry 2006:Glaxo SmithKline-Award for Outstanding Achievement in the field of Chemical Biology 2009: Member of the NRW Akademie der Wissenschaften und der Künste 2009: Member of the Akademie der Wissenschaften und der Literatur, Mainz 2010:Hans-Herloff Inhoffen-Medaille 2010 2011: Wilhelm-Manchot Research Professor- and Lectureship, TU Munich 2011:ERC Advanced Investigator Grant of the European Research Council under the European Union's Seventh Framework Programme (FP7/2007-2013) 2012: Visiting Fellow, Yale University, New Haven, USA 2012: Emil Fischer Medal of the GDCh (Gesellschaft Deutscher Chemiker) 2013-2016:Visiting Scientist at RIKEN, Japan 2015-2017:Cheney Fellowship, University of Leeds, UK 2016:Nauta Professor, VU Amsterdam Lectureships: 1) Eli Lilly Biocatalysis Lectureship, USA 1995 2) 3ème Cycle Lecturer, Schweiz 1996 3) Steinhofer Lectureship 1997 (Freiburg) 4) Merck Sharpe & Dohme Distinguished Lecturer, UK 1998 5) Zeneca Lectureship, UK 1999 6) Van de Kerk Lectureship, University of Utrecht, 2002 7) Amgen Lecturer, USA 2003 8) LEO Pharma Lecturer in Organic Chemistry, Denmark, 2005 9) ORGANON Lectureship, Glasgow, 2005 10) R. Raphael Lectureship, Glasgow, 2005 11) Roessler Lectures, Cornell University, Ithaca, USA, 2006 12) Musgrave Lectureship, Department of Chemistry, University of Durham, GB 2006 13) Bridget Ogilvie Lecture, School of Life Sciences, University of Dundee, GB, 2006 14) Melvin Calvin Lecture, UC Berkeley, USA, 2007 15) Cedric Hassall Lecture, Gregynog, GB, 2007 16) Solvay Pharmaceutical Lecture, Utrecht University, NL, 2007 17) The Evonik Lecture, University of Bristol, UK, 2008 18) IICT Hyderabad Foundation Day Lecture, India, 2008 19) Felix Serratosa Lecture, CSIC Barcelona, Spain, 2009 20) Wang Yu Memorial Lecture, SIOC, Shanghai, China, 2009 21) Merck-Frosst Lecture, Univ. of Alberta, Canada, 2009-2010 22) Eli Lilly Lecture, University of Illinois, USA, 2010 23) 35th Mellanby Memorial Lecture, CDRI, Lucknow, India, 2010 24) Merck Serono Lectureship, University of Nottingham, 2011 25) Chambers Lectureship, University of Rochester, USA, 2013 26) City University Distinguished Lecture, Hong Kong, China, 2013 27) Morningside Lecture in Chemical Biology, University of Hong Kong, China, 2013 28) H.C. Brown Lectures, Purdue University, USA, 2013 29) Novartis Lectureship, 2013 30) Novartis Chemical Sciences Lectureship, Harvard University, USA, 2015 31) Mendel Lecture, Masaryk University, Brno, Czech Republic, 2015 Member of the Editorial Board of international journals Member of the Kuratorium of “Angewandte Chemie “ Member of the Editorial Board of: • “Bioorganic and Medicinal Chemistry Letters” • “Bioorganic and Medicinal Chemistry” • “ChemBioChem” • “Chemical Biology & Drug Design” European Regional Editor of: “Bioorganic and Medicinal Chemistry” Chairman of the Executive Board of Editors for Tetrahedron Publications (2009-2010) Member of the Executive Board of Editors for Tetrahedron Publications Further professional activities: Scientific consultant to major pharmaceutical and agrochemical companies. Scientific consultant and Member of the Scientific Advisory Board of: • Taros Chemicals • HitGen Ltd, Chengdu, China Member of the Scientific Advisory Board of: • Max-Planck Innovation GmbH (Chair) • Boehringer Ingelheim Stiftung • Fakultät Pharmazie, Universität Marburg • Member of the General Assembly of Lead Discovery Center GmbH • Member of the Selection Committee for the Allocation of Alexander von Humboldt Foundation Research Awards • Member of the Kuratorium of the Fonds der Chemischen Industrie • Member of the “Beirat des Zentrums für Biomolekulare Wirkstoffe in Hannover” • Member of the Scientific Committee of the Helmholtz Zentrum für Infektionsforschung, Braunschweig • Member of the Scientific Committee of the Institut Européen de Chimie et Biologie, Bordeaux, France Close window Chemical Biological Modulation of KRas-Signaling
Jon Winter-Holt is a senior medicinal chemist working in the Oncology iMED at AstraZeneca.
Recently, he has led chemistry teams investigating a diverse range of oncology targets in the anti-invasive, cancer metabolism and cell signalling pathway areas, typically in early stage projects working up the output from high throughput screens. These targets include lactate dehydrogenase, glutaminase, monocarboxylate transporter 1, PFKFB3, MTH1, and the phosphatidylinositol-4, JAK1, and AXL kinases, on which he has published a number of papers, patent applications, and presentations. Jon earned a BSc(Hons) degree in chemistry at the University of Manchester in 1997, and continued to complete a PhD in synthetic organic chemistry working for Prof. Tim Donohoe on the directed dihydroxylation of allylic amides by osmium tetroxide. On joining AstraZeneca in 2001, Jon initially worked in the Respiratory and Inflammation Reaearch Area on chemokine inhibitors such as CCR5, CCR2, CXCR2, CXCR5, and CCR6 for rheumatoid and osteoarthritis, before moving to oncology in 2005. Close window Small Molecule Binding Sites on the RAS: SOS Complex Can Be Exploited for Inhibition of RAS Activation
Dr. Alfred Wittinghofer studied chemistry and worked as postdoc in UNC/US and Heidelberg, became a group leader in the Max Planck Institute (MPI) in Heidelberg in 1980.
From 1993 to 2009 he has been Director of the Department of Structural Biology at the MPI of Molecular Physiology in Dortmund. He has spent almost his entire scientific life on the elucidation of structure-function relationships of GTP-binding proteins. For the oncoprotein Ras he showed how it interacts with downstream components and its GTPase Activating Protein (GAP) and how it relates to oncogenic mutants. As an emeritus he uses an ERC advanced grant to work on Arl GTP-binding proteins and their involvement in ciliopathies. This work also led him to explore Ras drug candidates. Close window Studying Ciliary Trafficking and How it Leads to RAS Drug Candidates
Gail Wrigley is a Medicinal Chemistry Senior Research Scientist in the Oncology Innovative Medicines Biotech Unit at AstraZeneca, Cambridge, UK. Previously, Gail obtained a BSc(hons) in Natural Sciences from the University of Bath, including a year spent in industry working in the Combinatorial and Chemical Technologies Group of SmithKline Beecham, Harlow. She then continued her studies at The University of York, in the group of Professor RJK Taylor, obtaining a PhD in 2004. Directly after this, Gail joined the chemistry group of AstraZeneca, where she has worked on a wide range of drug projects from early lead generation through to candidate nomination, initially at Alderley Park, Cheshire and now in Cambridge. She was also a member of the medicinal chemistry team that discovered the approved EGFR inhibitor TagrissoTM.
Close window Advances in the Development of Covalent EGFR Inhibitors: from Early Hits to Osimertinib
Principal scientist, Project leader
I am working on neuroscience drug discovery, specifically Alzheimer’s Disease. As an organic chemist, I am also interested in fluorine chemistry due to its special position in drug discovery. We seek to discover new fluorination reagent and apply it in medicinal chemistry as well as PET chemistry for our late stage programm. 01/2002 – 05/2007 Ph.D. of Organic Chemistry at ETH Zürich 09/1994 – 07/1997 Ph.D. of Inorganic Chemistry at Nanjing University 10/2006 – 12/2007 Shanghai Givaudan Ltd Lab head, to discover new fragrance compounds with novel and unique odor. Close window Discovery of Brain-Penetrable LpPLA2 Inhibitor for Alzheimer’s Disease
Educational Background:
1997 B.Sc., Department of Chemistry, Fudan University
2003 Ph.D, Department of Chemistry, Princeton University (supervisor: Prof. John Groves)
203-2005 Postdoctoral Associate, Department of Chemistry, Yale University (supervisor: Andrew Hamilton)
Professional Career: 2008-present Principle Investigator, Professor, School of Pharmacy, Shanghai Jiao Tong University 2005-2007 Scientist, Anacor Pharmaceuticals, Palo Alto, California Research Interests: Our research focuses on two main themes: 1. Use small molecules as probes to elucidate unknown cellular events and therapeutic targets, and 2. Discover small molecule modulators of potential therapeutic targets. Awards 2014 WuXi Apptec Life Science and Chemistry Research Scholar Award 2008 New Century Excellent Talent Fund, Ministry of Education 2008 Shuguang Scholar Award 2008 Pujiang Talent Program Close window Chemical Biology Efforts in Cancer Drug Discovery Oral Communication
Neil Berry is a chemistry graduate of Exeter College, Oxford (1999) where he also obtained his DPhil (2002) in chemistry.
He moved to the University of Liverpool in 2003 as a post-doctoral research fellow in computational chemistry funded by Romark and in 2005 was appointed a University Teacher in Organic Chemistry whilst continuing his research. In 2007 he was appointed to a lectureship and in 2012 was promoted to senior lecturer. His principal research activities are in molecular modelling and chemoinformatics at the chemistry:biology interface and medicinal chemistry. A major focus is on anti-infective drug discovery with funded programs in the discovery and development of therapies for malaria, tuberculosis and chronic pain. He has been successful in attracting funding from EPSRC, MRC, ERC, Wellcome Trust, Bayer, International Vector Control Consortium, National Institute for Health Research and the Leverhulme trust. He has published >60 papers and patents to date and has collaborations with industry including AstraZeneca, Bayer, GSK and Unilever. Close window Anti-Wolbachia (A·WOL) Drug Discovery: Novel Hit Finding Via Ligand Based Virtual Screening Combined With HTS
Professor for Medicinal Chemistry / Drug Design
Eberhard Karls University Tübingen, Germany Scientific interests, current projects: - Molecular interactions and recognition, halogen / sigma hole bonding - Molecular design and fragment-based drug discovery (HEFLibs, Halogen-enriched fragment libraries) - Development of biophysical and computer-aided techniques - Structured therapeutic peptides, phage-encoded libraries - Innovative therapeutic concepts in oncology Education, Scientific Career: 2010 – today Professor (W3) for Medicinal Chemistry / Drug Design at Eberhard Karls University Tuebingen, Germany 2008 – 2010 Professor (W2 tenure track) for Pharmaceutical Chemistry / Bioanalytics at Ludwig Maximilians University Munich, Germany 2006 – 2008 Post-Doc, MRC Centre for Protein Engineering / Laboratory for Molecular Biology (Prof. Dr. Sir A. R. Fersht), Cambridge, UK 2004 – 2006 Habilitand at Pharmaceutical Institute, FAU Erlangen, Germany 2001 – 2004 Graduate studies / Ph. D. thesis (summa cum laude) in Pharmaceutical / Medicinal Chemistry at FAU Erlangen (Prof. Dr. P. Gmeiner) 2000 Research stay at the Laboratory for Behavioral Neurobiology at ETH Zürich (Prof. Dr. J. Feldon) 1995 – 1999 Studies of Pharmacy at Friedrich-Alexander University Erlangen-Nürnberg, Germany Close window EFMC Prize for a Young Medicinal Chemist in Academia
Intramolecular Hydrogen Bonds in the Design of CREBBP Bromodomain Ligands
Discovery of PF-06840003, a Novel IDO1 Inhibitor for Cancer Immunotherapy
Dr. Chris de Graaf is assistant professor computational medicinal chemistry at Vrije Universiteit Amsterdam.
Close window Mining Structural Protein-Ligand Interactions to Navigate Medicinal Chemistry Space
Daniela Digles studied Biotechnology with a specialisation on Chemistry of Active Substances at the University of Applied Sciences, FH-Campus Wien.
She completed her PhD studies at the University of Vienna, in the Pharmacoinformatics Research Group of Prof. Gerhard Ecker. The topic of her thesis was “Combined in silico/in vitro screening tools for identification of new insulin receptor ligands”, which she conducted with the help of a DOC-fFORTE-fellowship of the Austrian Academy of Sciences. In 2012 she started her Post-doc within the Open PHACTS project, where she is involved in testing the developed system, creating KNIME workflows to access the data to answer research questions, as well as user support. Since 2014, she is Senior Lecturer at the University of Vienna. Currently, her main research interests are the usage of Open Data, classification schemes, and the application of workflow tools. Close window Drug Targets in the Solute Carrier Classification (SLC)
Mr. Luiz Antonio Dutra
Position: PhD Student Institution of Research: School of Pharmaceutical Science, Araraquara, Sao Paulo State-Brazil Has Pharmacy’s Bachelor and drives research in Cardiovascular Diseases field. He has Master Degree position since 2013 from School of Pharmaceutical Science, Araraquara-Brazil, once designed and synthesized new antiplatelets and antithrombotic compounds. In 2014 he has started his PhD course at the same University, which is designing and synthesizing new PPARs receptors agonists. Since February 2016, makes a research exchange sponsored by Sao Research Foundation (Fapesp) at Department of Pharmaceutical Chemistry from Goethe University, Frankfurt-Germany, which is screening compounds as Bromodomains/PPARs inhibitors under supervision of Prof. Stefan Knapp. Close window Antiplatelet and Antithrombotic Activity of 1,2,5-Oxadiazole-2-N-Oxide Derivatives
Discovery of Ubrogepant (MK-1602): a Potent, Selective and Orally Bioavailable CGRP Receptor Antagonist for the Acute Treatment of Migraine
Gastreich holds a Diploma in Chemistry from Bonn University in Germany in 1996. After a research stay with Julian Gale at Imperial College in London, he earned his PhD in Theoretical Chemistry in Prof. Sigrid Peyerimhoff's department in Bonn modeling amorphous materials, and a minor in Bioinformatics from Prof. Thomas Lengauer at Fraunhofer in 2001.
Following a brief postdoc position at Düsseldorf University with Prof. Christel Marian, Gastreich joined BioSolveIT as Application Scientist in 2002 and became the organization's Principal Application Scientist in 2006. Since 2013 he oversees the Application Science at the company and is responsible for all interfacing between users and software development. His passion encompasses clear visualization tools, applied optimization, and conceiving of novel software to solve problems in drug design. He is (co-)author of several book contributions and various articles in the structure- and ligand-based arena as well as in fragment-based ligand design. Close window The evoSpace - A Synthesis-Driven Environment that Finds Accessible, Well-Behaved Compounds by Design
Antimo Gioiello received his PhD in Chemistry and Technology of Drugs from the University of Perugia (Italy) in 2005.
After post-doctoral experiences, in 2007 he was appointed Assistant Professor at the same university. Currently, he is Associate Professor of Synthetic and Medicinal Chemistry at the Department of Pharmaceutical Sciences (University of Perugia). His research work spans various stages from early discovery to clinical candidates in the area of liver and metabolic diseases. The main research interests of Antimo Gioiello include the development of chemical probes for understudied biological targets, implementation of enabling chemical technologies as flow chemistry to assist complex syntheses, design and optimization of new processing methods for compound library and large-scale preparation. He is a co-founder of TES Pharma, Perugia. Close window Atypical Bile Acids as Chemical Probes for Diagnosis and Therapy Monitoring of Progressive Cholestatic Liver Disease in HSD3B7 Patients
Xavier Gómez-Santacana recently obtained his PhD in Organic and Medicinal Chemistry at the University of Barcelona and the Institute for Advanced Chemistry of Catalonia (IQAC-CSIC) under the supervision of Prof. Amadeu Llebaria and Prof. Pau Gorostiza.
He has been working on the design, synthesis and pharmacological characterisation of photocromic ligands, which enable the on/off switching of metabotropic glutamate receptor activity in vitro an in vivo with light. He obtained his bachelor degree in 2008 and two MSc degrees (2010 and 2012). During his PhD studentship, he attended to several symposiums and was awarded with the best oral communication of the last edition of YMCS-EFMC. He also gained experience in industry in Almirall and Esteve Química (2008-2010). He currently has a position as a post-doc researcher in the division of Medicinal Chemistry of VU University, Amsterdam. Close window Photoisomerisable Allosteric Modulators Allow a Fine Control of mGlu Receptors with Light in Vivo (EFMC-YMCS Presentation Prize)
Senior Investigator within Global Discovery Chemistry at Novartis, with a specific focus on Neuroscience Medicinal Chemistry.
Mark gained his bachelor’s degree at the University of Liverpool in 1996 and PhD in 2001 at the University of Cambridge, UK, under the supervision of Professor Steven V Ley.
He worked in the team that discovered the Tyrosine Kinase inhibitor IRESSATM whilst at Zeneca Pharmaceuticals. He then contributed to a large number of drug discovery projects delivering clinical candidates in the pain and neuroscience disease areas at GlaxoSmithKline, including selective prostaglandin receptor antagonists and agonists, gamma secretase modulators and glycine transporter inhibitors. In 2010 he moved to Novartis in Horsham, UK, leading a number of respiratory projects including an inhaled prostacyclin receptor agonist for pulmonary arterial hypertension, which will commence it’s PhII PoC study this autumn. Since 2014 Mark hase worked at Novartis’ site in Cambridge, Boston, Massachusetts, supporting the Neuroscience Disease Area, contributing to a wide portfolio in particular to a novel antidepressant that is advancing towards clinic studies in 2017. Close window Optimising Membrane Interactions to Achieve Duration of Action for Inhaled Drug Candidates
• Name : Shalinee Jha
• Current title : M.Tech • Position : PhD in Biochemistry (Second year) • Supervisor : Prof. Dr. Peter Macheroux (Head, Institute of Biochemistry, Graz University of Technology) • Research field : Molecular Enzymology, Protein biochemistry, Murine model • Education : 2014 - PhD program DK Molecular Enzymology, Graz University of Technology, Austria 2012 - 2014 Master of Technology in Biotechnology, Indian Institute of Technology, Guwahati, India 2008 - 2012 Bachelor of Technology in Biotechnology, G B Pant University of Agriculture and Technology, Pantnagar, India • Professional experience: 05/ 2011 – 07/2011 Research Intern, Central Leather Research Institute, Chennai, India Close window Towards Low-Risk Painkillers: Human Dipeptidyl Peptidase III (hDPPIII) as a Novel Target for Therapeutic Pain Intervention
Dr Allan Jordan joined the CRUK Manchester Institute Drug Discovery Centre in July 2009 as Head of Chemistry.
He gained a BSc in Chemistry from UMIST in 1993 and, after a short spell as a teaching assistant in Arizona, he returned to UMIST to conduct post-graduate research into anticancer natural products. Following post-doctoral work at the University of Reading, he joined RiboTargets in Cambridge (now Vernalis) where he worked on for almost 10 years on a number of therapeutic areas at various stages of the research pipeline. He has been involved in the delivery of eight pre-clinical candidates, of which three have successfully entered human clinical trials. In his present role, alongside responsibilities for management of the chemistry team and progression of the drug discovery portfolio, he oversees the group’s capabilities in structural biology, computational chemistry and chemoinformatics. He additionally sites on several charity grant review bodies and acts as advisor for a number of charitable and non-for-profit drug discovery initiatives. As part of his role within Cancer Research UK, Allan is passionately involved in science communication and research engagement with the general public, fundraisers and technology providers, through direct contact and the broadcast media, receiving several awards and commendations from the charity for his efforts in this area. Close window Delivering First-in-Class In Vitro Chemical Probes Against Poly (ADP Ribose) Glycohydrolase (PARG)
Nir London, PhD. Senior Scientist (equivalent to Assistant Prof.)
Dept. of Organic Chemistry, The Weizmann Institute of Science.
Nir London received his PhD in computational structural biology from the Hebrew University of Jerusalem, Israel, in 2012. He then joined the group of Prof. Brian Shoichet at the University of California, San Francisco, for a post-doc.
He was awarded an EMBO long-term fellowship and the Program for Breakthrough Biomedic al Research award for his post-doctoral studies. In June 2015, he has started an independent research group at the Weizmann Institute of Science. Research in the lab is at the nexus of computation, chemistry and biology with a focus on the discovery and development of covalent chemical probes. Close window Rapid Discovery of Potent and Selective Covalent Inhibitors via Covalent Docking
Dr. Mapelli is Sr. Principal Scientist in the Department of Discovery Chemistry, Bristol-Myers Squibb, Princeton, NJ.
After receiving his doctoral degree in Organic Chemistry from the University of Padua in Italy, he moved to the US where he held post-doctoral appointments at the University of Georgia and University of Louisville from 1983 to 1988. He began his industrial career at EniChem Americas, where he worked in the biotech division. In 1991 he joined Bristol-Myers Squibb, where he has been since. His research interests include peptide-based medicinal chemistry, peptidomimetic therapeutics and chemical development of peptides. Dr. Mapelli is a co-inventor on seventeen patents and has co-authored more than thirty peer review papers. He is a reviewer for several journals including Organic Letters, Journal of Organic Chemistry, Journal of Medicinal Chemistry, Organic Process Research & Development. Close window Attempts at Oral Delivery of a Series of Short Unnatural Peptides: Still Like Pushing a Camel Through the Eye of a Needle?
Research Professor at CSIC (Spanish Council for Research). Head of Traslational Medicinal and Biological Chemistry Laboratory in the Biological Research Center (CSIC, Madrid).
Research fields: Drug discovery and development for central nervous system pathologies (neurodegenerative diseases, multiple sclerosis, autism,....). Education: Bs Organic Chemistry (1984, UCM, Madrid), Ms Medicinal Chemistry (1984, UCM, Madrid), PhD Medicinal Chemistry (1987, UCM, Madrid), Ms Bussiness (2005, IESE, UNav, Madrid). Professional experience: 1990 tenured scientist, Medicinal Chemistry Institute-CSIC; 2002-2007 R&D Director NeuroPharma; 2008 scientific researcher, Medicinal Chemistry Institute-CSIC; 2009-2013 Research Professor, Medicinal Chemistry Institute-CSIC; 2014 to date, Research Professor, Biological Research Center-CSIC. Author of more than 225 publications in scientific journals, more than 30 active patents in the pharmaceutical field, editor adn/or author of 6 books, Founder of ANKAR PHARMA Close window Systemic Administration of an Allosteric GSK-3 Inhibitor Delays Photoreceptor Cell Death and Preserves Visual Function in a Retinitis Pigmentosa Mouse Model
Leticia Monjas obtained her Bachelor's degree in Chemistry in 2010 from the Complutense University of Madrid, Spain. She spent her last year at the University of Groningen with an Erasmus fellowship, where she did her research project in the group of Prof. A. J Minnaard.
In 2012, she graduated from the Complutense University of Madrid with a Master in Organic Chemistry. She did her Master project at the Medicinal Chemistry Institute of CSIC (Spanish National Research Council), under the supervision of Dr. M. I. Rodriguez-Franco and Dr. S. Conde, working on the synthesis and biological evaluation of multifunctional compounds for the treatment of Alzheimer's disease. In September 2012, she started her PhD in the group of Prof. A. K. H. Hirsch, and her research interest lies in the field of design and synthesis of small-molecule modulators of essential transport functions in pathogenic bacteria. Close window Exploring Hit-Identification Strategies for Energy-Coupling Factor Transporters, a Novel Target for the Development of Antibiotics
Michaela Müller received her B.Sc. and her M.Sc. degree in Computational Life Science from the University of Lübeck, Germany in 2011 and 2013, respectively.
Since 2013, she is a PhD student at the Institute for Integrative and Experimental Genomics at the University of Lübeck, Germany. Her research interests involve in silico analysis of proteins associated with cardiovascular diseases, e.g., ADAMTS7, namely through homology modeling, molecular dynamics, structure-based drug design and virtual screening Close window Classification of Adamts Binding Sites: the First Step Toward Selective ADAMTS7 Inhibitors
Director, leading the Automation and Capabilities Enhancement (ACE) group in West Point PA
Broad background in medicinal chemistry, including HIV, neuroscience, pain, arthritis, and cardiovascular research. Expertise in therapeutics targeting proteases, kinases, GPCRs and ion channels. Diverse team leadership experience spans: Hit Identification, Lead Identification, Lead Optimization and Preclinical Development to Phase I Testing. Particular expertise with leveraging new technology to accelerate drug design and synthesis, for example parallel medicinal chemistry. Postdoctoral Research Associate with Professor K. C. Nicolaou at the Chemistry Department of the Scripps Research Institute, La Jolla, CA Ph.D., Organic Chemistry, March 1993, The University of North Carolina at Chapel Hill 3 years at Novartis US, 19 years at Merck, West Point, US. Close window Functionally Irreversible Non-Covalent Inhibitors of FAAH: a Safer Approach?
David is an Associate Director in the Medicinal Chemistry department at Astex Pharmaceuticals.
He studied Chemistry at the University of Southampton where he also completed his PhD in synthetic organic chemistry. He then started his career at GSK in Harlow in 2004 in the Neurology CEDD. David spent six years at GSK, where he worked on a number of target classes (GPCR’s, ion channels and enzymes) covering a range of indications including Alzheimer’s Disease, Multiple Sclerosis, cognitive impairment and neuropathic pain. David started at Astex in 2010, learning about fragment based drug discovery and structure based drug design. He was project leader for the Fragment Library for two years and has worked on successful collaboration projects with GSK along with internal projects on Hepatitis C infection and cancer. Close window From Fragment to in vivo Activity for a Challenging PPI Target: the Discovery of Potent Inhibitors of the KEAP1-NRF2 Interaction
Dr. Alleyn Plowright obtained his PhD in organic chemistry with Professor Gerald Pattenden at the University of Nottingham in 1999, and continued with postdoctoral studies with Professor Andrew Myers at Harvard University in 2000–2001.
In 2002, he joined AstraZeneca, UK as a medicinal chemist working in Oncology and then Metabolic Disease research areas. In 2006, he moved to AstraZeneca, Sweden, where he led the medicinal chemistry efforts in various drug discovery programs, before taking on the leadership of the lead optimization chemistry section. In 2012, he became Senior Principal Scientist, Medicinal Chemistry and a Project Leader in the Cardiovascular and Metabolic Diseases Innovative Medicines unit. His research interests include drug design, phenotypic screening, working with multiple chemical modalities and drug discovery including regenerative medicine. Close window Phenotypic Screening for the Discovery of Novel Molecules for Therapeutic Heart Regeneration
Jean Quancard studied Chemistry at Ecole Normale Superieure in Paris and stayed in Paris for a PhD in chemical biology at University of Pierre et Marie Curie.
In 2004, he moved to Stanford University in the US for a Postdoc with Pr. Barry Trost. Jean joined Novartis in 2006 in the Global Discovery Chemistry department as a Medicinal Chemistry Labhead and since then worked in several therapeutic areas such as autoimmunity, oncology, ophthalmology and neuroscience. He led several projects from exploratory to late stage optimization as well as pre-clinical development. Jean then spent two years as a chemistry group leader in the Autoimmunity and Neuroinflammation fields. Currently, Jean is head of chemistry for the Musculoskeletal disease area. Close window EFMC Prize for a Young Medicinal Chemist in Industry
Neil Ranson is Associate Professor of Structural Biology and Director of EM for the Astbury Biostructure Laboratory at the University of Leeds. He did a BSc in Biochemistry, followed by a PhD in mechanistic enzymology at the University of Bristol.
He cross trained into structural biology at Birkbeck College London, working with Professor Helen Saibil using cryo-EM to study conformational in molecular machines. He came to Leeds in 2002 as a University Research Fellow, His main interests are now in using cryo-EM to determine the 3-D structures of macromolecular assemblies. Current projects include structural virology (especially the structure and function of single-stranded RNA viruses), amyloid protein aggregation in disease (especially in neurodegeneration), and in the structure of membrane proteins. Close window How can Advances in Cryo-Electron Microscopy Revolutionize Medicinal Chemistry?
Orr Ravitz is the product manager of ChemPlanner, Wiley’s synthesis planning platform, and is leading the development and application of technologies in the areas of Computer Aided Synthesis Design and cheminformatics. Dr. Ravitz joined Wiley in 2014, when the company acquired SimBioSys, a Toronto-based software developer of computational chemistry applications, where he served as the product manager of ARChem, and as Chief Operating Officer.
Dr. Ravitz received his PhD in Chemical Physics from Columbia University, and a BSc in Chemistry and Physics from Tel Aviv University. Prior to joining SimBioSys he pursued post-doctoral research in Biophysics at the University of Rochester. Close window Identifying Synthetic Opportunities Using Chemplanner - How Computers Assist Chemists in Covering a Greater Synthetic Space
Christophe Rochais received his PhD with the group of Professor S. Rault from the University of Caen Basse-Normandie (2005). After completing a postdoctoral fellowship at the Centre for Biomolecular Sciences of the University of Nottingham (2007), under the supervision of Professor Peter M. Fischer, he was appointed lecturer in Organic Chemistry in the School of Pharmacy at the University of Caen in 2007.
Since January 2014, he has assumed the position of professor in Organic Chemistry. His research interests include medicinal chemistry in the field of enzymatic inhibition, as well as receptor modulation, in order to develop pharmacological tools and bioactive compounds. Since 2012 he has been leading a research program dedicated to the development of pleiotropic agents of interest in the treatment of Alzheimer's disease (PLEIAD). Close window Modulation of RS67,333: from a 5-HT4R Partial Agonist to the Identification of Several Promising Multi-Target Directed Ligands for Alzheimer's Disease
Eduardo Ruivo obtained his degree in Applied Chemistry in 2012 from the Faculty of Science and Technologies, New University of Lisbon (FCT-UNL), Portugal. He completed his Master degree in Medicinal Chemistry in 2014 at the Faculty of Pharmacy, University of Lisbon, where he was dedicated to the synthesis of new protease inhibitors and probing methodologies.
In the end of 2014 he was awarded with a research grant by AstraZeneca Foundation (Portugal) for the development of Activity-Based Probes Toward the Validation of Chronic Obstructive Pulmonary Disease Biomarkers. In 2015 he was invited for a PhD at the University of Antwerp in the Medicinal Chemistry group where he is currently devoted to the use of bioorthogonal chemistry together with antibody conjugation for in vivo cancer imaging, using positron emission tomography (PET) or single photon emission computed tomography (SPECT) imaging. Close window Novel Antibody-Tetrazine Conjugate for Breast Cancer Imaging
Dr. Volker K. Schulze is Senior Scientist at BAYER Pharma AG, Drug Discovery, Medicinal Chemistry Berlin.
Volker studied chemistry at the University of Marburg. As an Erasmus student he spent time in the laboratory of N.G. Connelly in Bristol, UK. In 1993 he received his diploma and in 1997 he completed his Ph.D. with Prof. R.W. Hoffmann in Marburg working on the mechanism and synthetic applications of an enantioselective halogen metal exchange reaction. He then joined the group of Prof. J.D. White in Corvallis, Oregon for a post-doctorate, working on the total synthesis of pyrrolizidine alkaloids. Volker started his industrial career at Albany Molecular Research in 1999 and then joined former Schering AG in 2001. He is currently a Senior Scientist at BAYER Pharma AG in Berlin, where he has worked on several Oncology projects in early hit to lead phase as well as in lead-structure optimization. Close window Driving Tumors into Mitotic Catastrophe - Lead Generation of MPS1 Inhibitors Leading to Two Clinical Candidates BAY 1161909 and BAY 1217389
Gisele Silvestre da Silva is currently a PhD student at Department of Organic Chemistry, UNICAMP, Brazil.
Her research interests include synthesis of prototypes that represent an opportunity to discover new drug candidates to treat Alzheimer’s disease. In this presented work, she synthesized acylhydrazones compounds that have been evaluated for their inhibitory effects on acetylcholinesterase (AChE) and on fibrillization of Aβ42 peptide. Close window Effects of Novel Acylhydrazones Derived From 4-Quinolone on the Acetylcholinesterase Activity and Aβ42 Peptide Fibrils Formation
Dr Graham F. Smith is currently director of Medicinal Chemistry at Merck Research Laboratories in Boston. He is active in the areas of small molecule lead discovery, chemical technologies and medicinal chemistry research.
He graduated from the University of Nottingham, UK and continued there to complete a PhD in natural product synthesis with Prof. Gerry Pattenden. He continued work in the area of natural product research at the Ohio State University under the guidance of Prof. Leo Paquette. He has worked as a medical chemist in the pharmaceutical industry in positions of increasing responsibility for over 20 years for Sanofi, Pfizer and Merck. Close window Non Coding RNA as a Small Molecule Druggable Target
First Disclosure of CDZ173 - Discovery of a New Generation of Potent and Selective PI3K Delta Inhibitors for Autoimmune and Inflammatory Diseases
Thomas Michael gained his first degree in chemistry in 1995 and his PhD in organic chemistry in 1999, both from the University of Strathclyde. He then worked for PanTherix as a medicinal chemist from 1999-2003: a biotech utilising SBDD for antibacterials.
After this he worked at Heriot-Watt university on an anti-HIV programme, followed by a senior medicinal chemistry position with Cyclacel in Dundee, working on cancer therapies, from 2006-2009. Thomas then moved to the Drug Discovery Unit at the University of Dundee, where he is currently the chemistry team-leader for the Kinetoplastids project, which is a collaboration with GSK, focussed on delivering new therapies for neglected tropical diseases. Close window The Development of DDD853651; a Potential Candidate for the Treatment of Visceral Leishmaniasis
Tihomir Tomašič studied pharmacy at the University of Ljubljana, Faculty of Pharmacy, Slovenia, where he obtained his Master degree in 2006 and his Ph. D. in pharmacy in 2011.
During his Ph. D. study, he visited the group of Prof. Dr. Gerhard Klebe at the Philipps Universität Marburg in Germany in 2008, where he worked on discovery of novel antibacterials using virtual screening. In 2012 he became an assistant professor at the Chair of Pharmaceutical Chemistry at the Faculty of Pharmacy, University of Ljubljana. His research interests involve mainly the computer-aided design and synthesis of biologically active compounds, particularly with antibacterial and antiviral activity. Close window Interaction of 4,5,6,7-Tetrahydrobenzo[1,2-D]Thiazoles with the Cellular Chaperone HSP90 as a Potential Pathway to Inhibit Hepatitis C Virus Replication
Dmitry Tsvelikhovsky obtained his Ph.D. degree in Chemistry from the Hebrew University of Jerusalem (Israel) in 2009, where he worked under the supervision of Prof. Jochanan Blum.
His graduate research explored the reactivity and synthetic applications of lanthanides.
He entered Massachusetts Institute of Technology (MIT) as a Postdoctoral Fellow in 2009, working with Prof. Stephen L. Buchwald. His projects focused on Pd-Catalyzed reactions, aiming to develop novel routes towards the synthesis of N- and O-containing heterocycles. In 2012 Dr. Tsvelikhovsky obtained the Assistant Professor position with the Institute for Drug Research, the Hebrew University of Jerusalem. His research efforts are revolving around discovery and design of advanced molecular intermediates, able to serve as common platforms for synthesis of various, structurally related compounds – potential therapeutic agents and drug candidates. Dr. Tsvelikhovsky has been recently awarded Marie Curie Career Integration Grant (CIG), German-Israeli Foundation Grant for Young Scientists (GIF) and the Volkswagen Stiftung Research Grant. Close window Rapid Composition of Tricyclic Spiranoid Lactones: Access to Natural Frames and Application in Selective Silencing of the Pain Receptor TRPV1
Dr. Mario van der Stelt (Associate Professor in Medicinal Chemistry) heads the Molecular Physiology group at Leiden University, the Netherlands (www.universiteitleiden.nl/en/science/chemistry/molphys).
The main theme in his group is the design, synthesis and application of small molecules as chemical tools to control and visualize proteins during (neuro)inflammation, metabolic syndrome and cancer. In multidisciplinary research lines medicinal chemistry is combined with chemical biology techniques, such as chemical proteomics and activity-based protein profiling. Previously, Dr. Van der Stelt worked as a medicinal chemist and leader of Lead Finding & Lead Optimization teams in the Merck Research Laboratories (from 2004-2012) in the Netherlands. Close window Discovery of In Vivo Active and Selective Diacylglycerol Lipase-Alpha Inhibitors |
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