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Lecture | Van Leeuwenhoek Lecture on BioScience

Cannabinoid receptor 2 agonists on their way to clinics – How industrial drug discovery and academic research can cross-fertilize each other

  • Uwe Grether (Basel, Roche Pharma Research and Early Development, Roche Innovation Center)
Thursday 28 November 2019
Gorlaeus Gebouw
Einsteinweg 55
2333 CC Leiden
LUMY 04.28

Uwe Grether is Senior Principal Scientist, Medicinal Chemistry, F. Hoffmann-La Roche, Basel. Uwe received his PhD in chemistry under the direction of Prof. Herbert Waldmann from the University of Karlsruhe in 2000. From 2000-2001  he carried out postdoctoral work in the laboratory of Prof. James White at the Oregon State University, Corvallis. In 2001, Uwe joined the Medicinal Chemistry section of F. Hoffmann-La Roche as a research chemist. Over the years he has contributed to a number of drug discovery programs for the treatment of metabolic, cardiovascular, kidney, neuroscience and more recently ophthalmic diseases. Uwe worked as team member and project leader covering both early and late stage research and reaching advanced stages up to phase 3 clinical trials. He is co-author of more than 100 patent applications and research publications.

On the example of the cannabinoid receptor 2 (CB2R) agonist project aiming for the treatment of kidney diseases, a small molecule drug discovery program will be discussed from project initiation toward advanced stage. During the evolution of the project several interesting scientific questions appeared which could efficiently be addressed by teaming up with academic partners. Mutually rewarding collaborations arose, giving rise to a number of scientific publications. The presentation will highlight various aspects of the CB2R program such as target validation, hit generation, lead optimization as well as in vitro and in vivo pharmacology profiling. Furthermore, the in depth profile of advanced molecules will be discussed. Finally, the generation and application of novel CB2R probes shall be presented, to illustrate the importance of chemical probes at all stages of drug discovery programs starting from receptor localization and trafficking studies toward biomarker applications.


Please keep the following dates free in your diary (all Thursdays at 16h.)

January 30 2020, Jonathan Bard (Oxford)
February 20 2020, Alexander Kros
March 26 2020, Thijs Ettema (WUR)
April 23 2020, Christian Kost (Osnabrück)
May 28 2020, Matthias Lutolf (Lausanne EFPL)
June 25 2020, Stan Awramik (Santa Barbara, Earth Science)

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