16th EFMC Short Course on Medicinal Chemistry

New Opportunities in GPCR Drug Discovery

 Oegstgeest (near Leiden), The Netherlands    May 8-11, 2022

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 Biology of GPCRs in the Era of Cryo-EM – Implications for Drug Design and Discovery

Dr Moran SHALEV-BENAMI
WEIZMANN INSTITUTE, Rehovot, Israel
12:30

Lunch

14:00

GPCR Ligands: Molecular Recognition, Kinetics and Allosteric Modulation

Prof. Laura HEITMAN
UNIVERSITY OF LEIDEN, Leiden, The Netherlands
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

A General Introduction into GPCRdb & Hands-on with the GPCRdb

Dr Albert KOOISTRA
UNIVERSITY OF COPENHAGEN, København, Denmark
10:30

Coffee Break

11:00

System Biology Approaches to GPCR Targets

Dr Aurelien RIZK
INTERAX BIOTECH, Villigen, 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

Tutorials and Excercises

Dr Chris DE GRAAF
SOSEI HEPTARES, Cambridge, United Kingdom
Dr Albert KOOISTRA
UNIVERSITY OF COPENHAGEN, København, Denmark
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

Discovery of H1/H4 Dual Ligands

Prof. Iwan DE ESCH
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands
10:30

Coffee break

11:00

Binding and Modulating GPCRs by Inside/Outside Binding Nanobodies

Dr Raimond HEUKERS
QVQ, Utrecht, The Netherlands
12:30

Wrap up and Lunch