16th EFMC Short Course on Medicinal Chemistry
Sunday May 8, 2022
17:00Registration
19:00Dinner and Get Together
Monday May 9, 2022
07:30Breakfast
08:30Opening
09:00General Introduction to GPCRs: Pharma Relevance, Indications, Molecular Pharmacology
Prof. Rob LEURS
(VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands)
10:30Coffee Break
11:00Structural Biology of GPCRs in the Era of Cryo-EM – Implications for Drug Design and Discovery
Dr Moran SHALEV-BENAMI
(WEIZMANN INSTITUTE, Rehovot, Israel)
12:30Lunch
14:00GPCR Ligands: Molecular Recognition, Kinetics and Allosteric Modulation
Prof. Laura HEITMAN
(UNIVERSITY OF LEIDEN, Leiden, The Netherlands)
15:30Coffee Break
16:00Partial Agonism/Biased Signalling and its Therapeutical Relevance
Dr Rob LANE
(UNIVERSITY OF NOTTINGHAM, Nottingham, United Kingdom)
17:30Day End
18:00Walking tour through Leiden
19:00Dinner in Leiden
Tuesday May 10, 2022
07:30Breakfast
08:30A General Introduction into GPCRdb & Hands-on with the GPCRdb
Dr Albert KOOISTRA
(UNIVERSITY OF COPENHAGEN, København, Denmark)
10:30Coffee Break
11:00System Biology Approaches to GPCR Targets
Dr Aurelien RIZK
(INTERAX BIOTECH, Villigen, Switzerland)
12:30Lunch
14:00GPCR Ligand Design: Cheminformatics and Modelling
Dr Chris DE GRAAF
(SOSEI HEPTARES, Cambridge, United Kingdom)
15:30Coffee Break
16:00Tutorials and Excercises
Dr Chris DE GRAAF (SOSEI HEPTARES, Cambridge, United Kingdom)
Dr Albert KOOISTRA (UNIVERSITY OF COPENHAGEN, København, Denmark)
18:30Day End
19:00Dinner and Get Together
Wednesday May 11, 2022
07:30Breakfast
08:30Discovery of Cariprazine, A Dopamine D3 Receptor Prefering Third Generation Antipsychotics
Prof. György KESERU
(HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary)
09:30Discovery of H1/H4 Dual Ligands
Prof. Iwan DE ESCH
(VU AMSTERDAM, Amsterdam, The Netherlands)
10:30Coffee break
11:00Binding and Modulating GPCRs by Inside/Outside Binding Nanobodies
Dr Raimond HEUKERS
(QVQ, Utrecht, The Netherlands)
12:30Wrap up and Lunch

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