EFMC-ACSMEDI MedChem Frontiers 2019

Joint Symposium on Medicinal Chemistry Frontiers

 Krakow, Poland    June 10-13, 2019

Programme


10:00

Optional Excursions

15:00

Registration

17:30

Opening 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

17:45

Derivatives 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

18:30

Welcome Reception

08:00

Registration

Matrix Metallo-Proteinases

Session Chair

Prof. Krzysztof JOZWIAK
MEDICAL UNIVERSITY OF LUBLIN, Lublin, Poland

09:00

Libraries 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

09:30

MMP-9 at the Synapse in the Brain and Mind (IL02)

Prof. Leszek KACZMAREK
NENCKI INSTITUTE OF EXPERIMENTAL BIOLOGY, Warsaw, Poland

10:00

Metalloproteinase Cleavage Control of Interferon Alpha and Gamma Dampens Inflammation and Anti-Viral Immunity (IL03)

Prof. Christopher OVERALL
UNIVERSITY OF BRITISH COLUMBIA, Vancouver, Canada

10:30

Coffee Break and Exhibition

Genomics in Drug Discovery : Roles for Chemistry

Session Chair

Prof. Terry MOORE
UNIVERSITY OF ILLINOIS, Chicago, United States

11:00

Designing Synthetic Gene Regulators (SynGRs) (IL04)

Prof. Aseem ANSARI
UNIVERSITY OF WISCONSIN-MADISON, Madison, United States

11:30

Exploring Bacterial Genomes for Natural Product Discovery and Development (IL05)

Prof. Alessandra S. EUSTAQUIO
UNIVERSITY OF ILLINOIS AT CHICAGO, Chicago, United States

12:00

Integrative Screening Identifies a Novel Node in the Oncogenic YAP/HIPPO Pathway (IL06)

Dr Mathias FREDERIKSEN
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH (NIBR), Basel, Switzerland

12:30

Lunch and Exhibition

Advances in Protein Degradation Technologies

Session Chair

Prof. Daniel HARKI
UNIVERSITY OF MINNESOTA, Minneapolis, United States

14:00

Targeted Protein Degradation with Small Molecules: how PROTACs Work (IL07)

Prof. Alessio CIULLI
UNIVERSITY OF DUNDEE, Dundee, United Kingdom

14:30

The Ubiquitin System (IL08)

Prof. Huib OVAA
LEIDEN UNIVERSITY MEDICAL CENTER, Leiden, The Netherlands

15:00

Small-Molecule Modulation of Cereblon Protein Level (OC01)

Mr Christian STEINEBACH
UNIVERSITY OF BONN, Bonn, Germany

15:15

Drugging Challenging E3 Ligases: A Novel Multidisciplinary Approach to Identify Small-Molecules that Bind FBW7 (OC02)

Ms Miriam MARTINEZ CARTRO
UNIVERSITY OF BARCELONA, Barcelona, Spain

15:30

Coffee Break and Exhibition

Session Chair

Prof. Andrzej BOJARSKI
INSTITUTE OF PHARMACOLOGY POLISH ACADEMY OF SCIENCES, Krakow, Poland

16:00

Systems Pharmacology Links GPCRs with Retinal Degenerative Disorders (PL02)

Prof. Krzysztof PALCZEWSKI
CASE WESTERN RESERVE UNIVERSITY, Cleveland, United States

16:45

First 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

17:15

Poster Session 1
(Posters with odd numbers)

GPCRs: a Discovery Powerhouse

Session Chair

Dr Yves P. AUBERSON
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland

09:00

G Protein-Coupled Receptors: the Structural Basis for their Pharmacology (IL10)

Dr Chris TATE
MRC LABORATORY OF MOLECULAR BIOLOGY, Cambridge, United Kingdom

09:30

Design of Orexin-1 Receptor Selective Antagonists (IL11)

Dr Uta LESSEL
BOEHRINGER INGELHEIM, Biberach an der Riss, Germany

10:00

Next Generation GPR119 Agonists as Potential Treatment for Cardiometabolic Diseases (IL12)

Dr Lothar SCHWINK
SANOFI, Frankfurt Am Main, Germany

10:30

Coffee Break and Exhibition

Specific and Multi-Targeted Drugs

Session Chair

Prof. Andrzej BOJARSKI
INSTITUTE OF PHARMACOLOGY POLISH ACADEMY OF SCIENCES, Krakow, Poland

11:00

Charting New Paths in Multi-Target Drug Discovery for Alzheimer’s Disease (IL13)

Prof. Maria Laura BOLOGNESI
UNIVERSITY OF BOLOGNA, Bologna, Italy

11:30

Multiple Targeting - The Histamine H3 Receptor Pharmacophore as Central Element (IL14)

Prof. Holger STARK
HEINRICH HEINE UNIVERSITY DÜSSELDORF, Duesseldorf, Germany

12:00

Chemical Biology for Drug Discovery: A Click and Play Approach Exemplified by ERK1/2 Probes (OC03)

Dr Charlotte GRIFFITHS-JONES
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom

12:15

Identification 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

12:30

Lunch and Exhibition

Opioid, Pain, Endo-Cannabinoid

Session Chair

Prof. Katarzyna KIEC-KONONOWICZ
JAGIELLONIAN UNIVERSITY, Krakow, Poland

14:00

Cannabinoid 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

14:30

Potential of Natural Cannabinoids and Synthetic Cannabinoids in Neuroprotection (IL16)

Prof. Rafael FRANCO
UNIVERSITY OF BARCELONA, Barcelona, Spain

15:00

Discovery 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

15:15

The Discovery and Development of the Clinical FAAH Inhibitor JNJ-42165279 (OC06)

Prof. James BREITENBUCHER
UNIVERSITY OF CALIFORNIA SAN FRANCISCO, San Francisco, United States

15:30

Coffee Break and Exhibition

16:00

Next 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

Pharma Research Highlights in Poland

16:45

Discovery 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

17:00

DPD-inspired Small Heterocyclic Libraries Characterized as Novel LsrK Kinase Inhibitors: an Opportunity to Fight Antimicrobial Resistance (OC08)

Dr Anna KARAWAJCZYK
SELVITA, Krakow, Poland

17:15

Poster Session 2
(Posters with even numbers)

20:00

Symposium Banquet

Chemical Biology Tools & Target Engagement Technologies

Session Chair

Prof. Edgars SUNA
LATVIAN INSTITUTE OF ORGANIC SYNTHESIS, Riga, Latvia

09:00

Protein-Ligand Interactions: How Medicinal Chemistry Contributes to the Understanding of Molecular Recognition (IL17)

Dr Marc NAZARE
FMP, Berlin, Germany

09:30

Adventures in Targeting Protein Lipdation: Breaking Drug Resistance Using Fragment Deconstruction and Chemical Biology (IL18)

Prof. Edward TATE
IMPERIAL COLLEGE LONDON, London, United Kingdom

10:00

Chemical Physiology of Antibody Conjugates and Natural Products (IL19)
"2018 MedChemComm Emerging Investigator Lectureship"

Dr Goncalo BERNARDES
INSTITUTO DE MEDICINA MOLECULAR, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom

10:30

Coffee Break and Exhibition

Targeted Covalent Inhibitors

Session Chair

Dr. Anders KARLÉN
UPPSALA UNIVERSITY, Uppsala, Sweden

11:00

Safety First: Covalent Inhibitors from a Safety Perspective (IL20)

Dr Mickael MOGEMARK
ASTRAZENECA, Mölndal, Sweden

11:30

Adventures in Functional Assignment and Inhibition of Metallo-Enzymes (IL21)

Prof. Christopher J. SCHOFIELD
UNIVERSITY OF OXFORD, Oxford, United Kingdom

12:00

Mining the Protein Kinase Cysteinome (IL22)

Dr Tjeerd BARF
ACERTA PHARMA BV, Oss, The Netherlands

12:30

Lunch and Exhibition

Adding AI to the Drug Discovery Tool Box

Session Chair

Dr Carolyn DZIERBA
BRISTOL-MYERS SQUIBB, Wallingford, United States

14:00

Learning the Art of Chemical Synthesis with Deep Neural Networks and Discipline Scale Data (IL23)

Prof. Mark WALLER
UNIVERSITY OF WOLLONGONG, Wollongong, Australia

14:30

Applications of Artificial Intelligence in Drug Discovery – Separating Hype From Utility (IL24)

Dr Pat WALTERS
RELAY THERAPEUTICS, Cambridge, United States

15:00

Augmented Intelligence for Compound Design (OC09)

Dr Michal WARCHOL
ARDIGEN, Krakow, Poland

15:15

Capturing and Applying Knowledge to Guide Compound Optimisation (OC10)

Mr Nick FOSTER
OPTIBRIUM, Cambridge, United Kingdom

15:30

Closing Remarks