16th EFMC Short Course on Medicinal Chemistry

New Opportunities in GPCR Drug Discovery

 Oegstgeest (near Leiden), The Netherlands    May 17-20, 2020

Programme


17:00

Registration

19:00

Dinner and Get Together

07:30

Breakfast

08:30

Opening

09:00

General Introduction to GPCRs: Pharma Relevance, Indications, Molecular Pharmacology

Prof. Rob LEURS
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands

10:30

Coffee Break

11:00

Structural Biochemistry of GPCRs

Dr Chris DE GRAAF
SOSEI HEPTARES, Cambridge, United Kingdom

12:30

Lunch

14:00

GPCR Ligands: Molecular Recognition, Kinetics and Allosteric Modulation

Dr Rob LANE
UNIVERSITY OF NOTTINGHAM, Nottingham, United Kingdom

15:30

Coffee Break

16:00

Partial Agonism/Biased Signalling and its Therapeutical Relevance

Dr Rob LANE
UNIVERSITY OF NOTTINGHAM, Nottingham, United Kingdom

17:30

Day End

18:00

Walking tour through Leiden

19:00

Dinner in Leiden

07:30

Breakfast

08:30

Tutorial and Excercise on GPCRdb

Dr Albert KOOISTRA
RADBOUD UMC NIJMEGEN, Nijmegen, The Netherlands

11:00

Coffee Break

11:30

System Biology Approaches to GPCR Targets

Dr Maria WALDHOER
INTERAX BIOTECH, Zürich, Switzerland

12:30

Lunch

14:00

GPCR Ligand Design: Cheminformatics and Modelling

Dr Chris DE GRAAF
SOSEI HEPTARES, Cambridge, United Kingdom

15:30

Coffee Break

16:00

Tutorial and Excercise

Dr Chris DE GRAAF
SOSEI HEPTARES, Cambridge, United Kingdom

18:30

Day End

19:00

Dinner and Get Together

07:30

Breakfast

08:30

Discovery of Cariprazine, A Dopamine D3 Receptor Prefering Third Generation Antipsychotics

Prof. Gyorgy KESERU
HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary

09:30

Case Study: Discovery of H1/H4 Dual Ligands

Prof. Iwan DE ESCH
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands

10:30

Coffee break

12:00

Case Study: Antibody Based Approaches

Dr Raimond HEUKERS
QVQ, Utrecht, The Netherlands

13:00

Wrap up and Lunch