This intensive course is intended for scientists working in the field, and the presentations will be given by senior scientists from industry and academia. The number of participants is limited to 35, to allow in depth discussion. Should the number of applications exceed the maximum, preference will be given to applicants from EFMC adhering countries and employees of EFMC corporate members. Upon special request to the organisers, only based on financial conditions and supported by an argued recommendation of the head of the department of the applicant, up to 3 applicants from academia may be admitted at a reduced fee.
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
Local Organisers
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)
