Uwe Grether

F. Hoffmann-La Roche, Switzerland

Title: Cannabinoid Receptor 2 Agonists on Their Way to Clinics – Cross-Fertilization of Industrial Drug Discovery and Academic Research

---

Biography

Uwe M. Grether, Expert Scientist, Medicinal Chemistry, F. Hoffmann-La Roche, Ltd. Basel, Switzerland. Uwe received his Ph.D. 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 D. White at the Oregon State University, Corvallis, OR. In 2001, Uwe joined the Medicinal Chemistry section of F. Hoffmann-La Roche, Ltd. Basel, Switzerland 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, ophthalmic and inflammatory 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 130 patents, research publications and book chapters.

Abstract

The type 2 cannabinoid receptor (CB2R) plays an important role in cell migration and immunosuppression and is therefore a promising GPCR drug target for the treatment of tissue injury and inflammation including kidney diseases. During the evolution of Roche’s CB2R agonist drug discovery program several challenging scientific questions appeared which could efficiently be addressed by teaming up with academic partners, leading to mutually rewarding collaborations. The presentation will highlight some of them and will illustrate different snapshots of Roche’s CB2R program. Both, early aspects such as target validation and hit generation as well as advanced stages including lead optimization and in depth in vitro and in vivo pharmacology profiles of advanced molecules will be covered. In addition, the generation and application of novel CB2R probes will be presented, to illustrate the importance of chemical probes at all stages of drug discovery programs starting from receptor localisation and trafficking studies toward biomarker applications.