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16th EFMC Short Course on Medicinal Chemistry: New Opportunities in GPCR Drug Discovery

17 May 2020 17:00 - 20 May 2020 14:00, Oegstgeest, Netherlands


Introduction
Course Outline

G-protein coupled receptors represent the largest class of drug targets. Although they serve as targets for about 30% of the known drugs, many of them is still orphan. In the last 15 years, however, we witnessed dramatic developments in the structural biology and pharmacology of GPCRs. High resolution X-ray and cryo-EM structures made the design of the GPCR ligands more rational. The widening knowledge on their signalling resulted in new concepts such as allosteric modulation, GPCR residence time and biased signalling currently tested in clinical trials. This course will provide an introduction for medicinal chemists to this important target class including concepts and methods applied in the structural biology, modelling, systems biology, pharmacology and medicinal chemistry of GPCRs.  The course will finish with a series of medicinal chemistry case studies, including the discovery of molecular probes, tool compounds, clinical candidates and marketed drugs.

Course Organisers
  • György Miklós KESERÜ (Research Centre for Natural Sciences, Hungarian Academy of Sciences, Hungary)
  • Rob LEURS (Vrije Universiteit Amsterdam, The Netherlands)

Local Organisers
  • Henk TIMMERMAN (Vrije Universiteit Amsterdam, The Netherlands)
  • Laura HEITMAN (University of Leiden, The Netherlands)
Venue
Castle Oud Poelgeest

Castle Oud Poelgeest, Poelgeesterweg 1, Oegstgeest, 2341 NM, Netherlands

Organised by
Contact information
Brieuc Matagne
LD Organisation
Rue Michel de Ghelderode 33/2
B-1348, Louvain-la-Neuve
Belgium
0472314984
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