EFMC-ACSMEDI MedChem Frontiers 2019
Monday June 10, 2019
10:00Optional Excursions
15:00Registration
17:30Opening of the Symposium & Welcome Address
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
Session Chair
Prof. Katarzyna KIEC-KONONOWICZ
(JAGIELLONIAN UNIVERSITY, Krakow, Poland)
17:45Derivatives of 1,3,5-triazine as a New Trend in the Search for the 5-HT6 Receptor Ligands with Therapeutic Perspectives (PL01)
Dr Jadwiga HANDZLIK
(MEDICAL COLLEGE OF JAGIELLONIAN UNIVERSITY, Krakow, Poland)
18:30Welcome Reception
Tuesday June 11, 2019
08:00Registration
Matrix Metallo-Proteinases
Session Chair
Prof. Krzysztof JOZWIAK
(MEDICAL UNIVERSITY OF LUBLIN, Lublin, Poland)
09:00Libraries of Fluorogenic Substrates with Natural and Unnatural Amino Acids as a Tool in Design of Active and Specific Probes for Investigation of Proteolytic Enzymes (IL01)
Prof. Marcin DRAG
(WROCLAV UNIVERSITY OF TECHNOLOGY, Wroclaw, Poland)
09:30MMP-9 at the Synapse in the Brain and Mind (IL02)
Prof. Leszek KACZMAREK
(NENCKI INSTITUTE OF EXPERIMENTAL BIOLOGY, Warsaw, Poland)
10:00Metalloproteinase Cleavage Control of Interferon Alpha and Gamma Dampens Inflammation and Anti-Viral Immunity (IL03)
Prof. Christopher OVERALL
(UNIVERSITY OF BRITISH COLUMBIA, Vancouver, Canada)
10:30Coffee Break and Exhibition
Genomics in Drug Discovery : Roles for Chemistry
Session Chair
Prof. Terry MOORE
(UNIVERSITY OF ILLINOIS, Chicago, United States)
11:00Designing Synthetic Gene Regulators (SynGR) (IL04)
Prof. Aseem ANSARI
(UNIVERSITY OF WISCONSIN-MADISON, Madison, United States)
11:30Exploring Bacterial Genomes for Natural Product Discovery and Development (IL05)
Prof. Alessandra S. EUSTAQUIO
(UNIVERSITY OF ILLINOIS AT CHICAGO, Chicago, United States)
12:00Integrative Screening Identifies a Novel Node in the Oncogenic YAP/HIPPO Pathway (IL06)
Dr Mathias FREDERIKSEN
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH (NIBR), Basel, Switzerland)
12:30Lunch and Exhibition
Advances in Protein Degradation Technologies
Session Chair
Prof. Daniel HARKI
(UNIVERSITY OF MINNESOTA, Minneapolis, United States)
14:00Targeted Protein Degradation with Small Molecules: how PROTACs Work (IL07)
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
14:30The Ubiquitin System (IL08)
Prof. Huib OVAA
(LEIDEN UNIVERSITY MEDICAL CENTER, Leiden, The Netherlands)
15:00Small-Molecule Modulation of Cereblon Protein Level (OC01)
Mr Christian STEINEBACH
(UNIVERSITY OF BONN, Bonn, Germany)
15:15Drugging Challenging E3 Ligases: A Novel Multidisciplinary Approach to Identify Small-Molecules that Bind FBW7 (OC02)
Ms Miriam MARTINEZ CARTRO
(UNIVERSITY OF BARCELONA, Barcelona, Spain)
15:30Coffee Break and Exhibition
Session Chair
Prof. Andrzej BOJARSKI
(INSTITUTE OF PHARMACOLOGY POLISH ACADEMY OF SCIENCES, Krakow, Poland)
16:00Systems Pharmacology Links GPCRs with Retinal Degenerative Disorders (PL02)
Prof. Krzysztof PALCZEWSKI
(CASE WESTERN RESERVE UNIVERSITY, Cleveland, United States)
16:45First Time Disclosure
The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders (IL09)
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
17:15Poster Session 1
(Posters with odd numbers)
18:15City Tour
Wednesday June 12, 2019
08:59GPCRs: a Discovery Powerhouse
Session Chair
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
09:00G Protein-Coupled Receptors: the Structural Basis for their Pharmacology (IL10)
Dr Chris TATE
(MRC LABORATORY OF MOLECULAR BIOLOGY, Cambridge, United Kingdom)
09:30Design of Orexin 1 Receptor Selective Antagonists (IL11)
Dr Uta LESSEL
(BOEHRINGER INGELHEIM, Biberach an der Riss, Germany)
10:00Next Generation GPR119 Agonists as Potential Treatment for Cardiometabolic Diseases (IL12)
Dr Lothar SCHWINK
(SANOFI, Frankfurt Am Main, Germany)
10:30Coffee Break and Exhibition
Specific and Multi-Targeted Drugs
Session Chair
Prof. Andrzej BOJARSKI
(INSTITUTE OF PHARMACOLOGY POLISH ACADEMY OF SCIENCES, Krakow, Poland)
11:00Charting New Paths in Multi-Target Drug Discovery for Alzheimer’s Disease (IL13)
Prof. Maria Laura BOLOGNESI
(UNIVERSITY OF BOLOGNA, Bologna, Italy)
11:30Multiple Targeting - The Histamine H3 Receptor Pharmacophore as Central Element (IL14)
Prof. Holger STARK
(HEINRICH HEINE UNIVERSITY DÜSSELDORF, Duesseldorf, Germany)
12:00Chemical Biology for Drug Discovery: A Click and Play Approach Exemplified by ERK1/2 Probes (OC03)
Dr Charlotte GRIFFITHS-JONES
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom)
12:15Identification and in-vivo Efficacy Studies of a Nicotinamide Derivative as Novel NNMT Inhibitor (OC04)
Dr Sven RUF
(SANOFI-AVENTIS DEUTSCHLAND GMBH, Frankfurt am Main, Germany)
12:30Lunch and Exhibition
Opioid, Pain, Endo-Cannabinoid
Session Chair
Prof. Katarzyna KIEC-KONONOWICZ
(JAGIELLONIAN UNIVERSITY, Krakow, Poland)
14:00Cannabinoid Receptor Type 2 Modulation to Improve Outcomes for Cartilage Repair in the Osteoarthritic Joint (IL15)
Prof. Katarzyna STAROWICZ-BUBAK
(INSTITUTE OF PHARMACOLOGY, POLISH ACADEMY OF SCIENCES, Krakow, Poland)
14:30Potential of Natural Cannabinoids and Synthetic Cannabinoids in Neuroprotection (IL16)
Prof. Rafael FRANCO
(UNIVERSITY OF BARCELONA, Barcelona, Spain)
15:00Discovery of Best in-class, Novel, Selective, Potent and Peripheral FLT3 Inhibitors, a New Way to Treat Neuropathic Pain (OC05)
Dr Dominique SURLERAUX
(BCI PHARMA, Liège, Belgium)
15:15The Discovery and Development of the Clinical FAAH Inhibitor JNJ-42165279 (OC06)
Prof. James BREITENBUCHER
(UNIVERSITY OF CALIFORNIA SAN FRANCISCO, San Francisco, United States)
15:30Coffee Break and Exhibition
Session Chair
Prof. Terry MOORE
(UNIVERSITY OF ILLINOIS, Chicago, United States)
16:00Next Generation Pain Therapeutics for the Opioid Crisis: Design of Bifunctional Nociceptin/Mu Opioid GPCR Ligands as non-Addicting Analgesics (PL03)
Dr Nurulain ZAVERI
(ASTRAEA THERAPEUTICS, Mountain View, United States)
16:45Pharma Research Highlights in Poland
16:45Discovery of OAT-2068 - A Potent, Selective, Orally Bioavailable Inhibitor of Mouse Chitotriosidase and its In Vivo Activity in the Bleomycin-Induced Pulmonary Fibrosis Model in Mice (OC07)
Dr Agnieszka BARTOSZEWICZ
(ONCOARENDI THERAPEUTICS SA, Warszawa, Poland)
17:00DPD-inspired Small Heterocyclic Libraries Characterized as Novel LsrK Kinase Inhibitors: an Opportunity to Fight Antimicrobial Resistance (OC08)
Dr Anna KARAWAJCZYK
(SELVITA, Krakow, Poland)
17:15Poster Session 2
(Posters with even numbers)
18:15End of Poster Session
20:00Symposium Banquet
Thursday June 13, 2019
Chemical Biology Tools & Target Engagement Technologies
Session Chair
Prof. Edgars SUNA
(LATVIAN INSTITUTE OF ORGANIC SYNTHESIS, Riga, Latvia)
09:00Protein-Ligand Interactions: How Medicinal Chemistry Contributes to the Understanding of Molecular Recognition (IL17)
Dr Marc NAZARE
(FMP, Berlin, Germany)
09:30Adventures in Targeting Protein Lipdation: Breaking Drug Resistance Using Fragment Deconstruction and Chemical Biology (IL18)
Prof. Edward TATE
(IMPERIAL COLLEGE LONDON, London, United Kingdom)
10:00Tankyrase Inhibitors : Evidence for Therapeutic Potential in Immuno-Oncology
Dr Luc VAN HIJFTE
(SCT & MERCACHEM-SYNCOM, Nijmegen, The Netherlands)
10:30Coffee Break and Exhibition
Targeted Covalent Inhibitors
Session Chair
Dr. Anders KARLÉN
(UPPSALA UNIVERSITY, Uppsala, Sweden)
11:00Safety First: Covalent Inhibitors from a Safety Perspective (IL20)
Dr Mickael MOGEMARK
(ASTRAZENECA, Mölndal, Sweden)
11:30Adventures in Functional Assignment and Inhibition of Metallo-Enzymes (IL21)
Prof. Christopher J. SCHOFIELD
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
12:00Mining the Protein Kinase Cysteinome (IL22)
Dr Tjeerd BARF
(ACERTA PHARMA BV, Oss, The Netherlands)
12:30Lunch and Exhibition
Adding AI to the Drug Discovery Tool Box
Session Chair
Dr Carolyn DZIERBA
(BRISTOL-MYERS SQUIBB, Wallingford, United States)
14:00Learning the Art of Chemical Synthesis with Deep Neural Networks and Discipline Scale Data (IL23)
Prof. Mark WALLER
(UNIVERSITY OF WOLLONGONG, Wollongong, Australia)
14:30Applications of Artificial Intelligence in Drug Discovery – Separating Hype From Utility (IL24)
Dr Pat WALTERS
(RELAY THERAPEUTICS, Cambridge, United States)
15:00Augmented Intelligence for Compound Design (OC09)
Dr Michal WARCHOL
(ARDIGEN, Krakow, Poland)
15:15Capturing and Applying Knowledge to Guide Compound Optimisation (OC10)
Mr Nick FOSTER
(OPTIBRIUM, United Kingdom)
15:30Closing Remarks

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