In the past, drugs have been discovered either by identifying the active principle from traditional remedies or by serendipitous discovery. Contemporary approaches focus on a clear understanding of how diseases are controlled at the molecular level in order to target specific entities based on this knowledge. Insights about structure and function of proteins involved in pathophysiological processes are crucial for success. The process of drug discovery involves the identification of molecular targets, drug candidates, synthetic optimization of lead structures, their functional characterization, and hence the development of suitable assays to test for therapeutic efficacy prior to clinical trials. This embarks both in vitro and in vivo models.

In collaboration with Prof. Karl-Heinz Altmann, Gertsch was involved in the development of highly active microtubule-stabilizing agents both as tool compounds and potential drug candidates (Gertsch et al., 2009, ChemBioChem 10, 2513; Feyen et al. 2008, Acc. Chem. Res. 41, 21; Altmann & Gertsch, Nat. Prod. Rep. 24, 327).

The Gertsch group is interested in chemical biology in drug discovery with a focus on signal transduction and inflammation. A major focus of the Gertsch group is the endocannabinoid system (ECS) for drug discovery. Currently, the CB2 cannabinoid receptor (Markt et al., 2009, J. Med. Chem. 52, 369; Gertsch et al., 2008, PNAS, 105, 9099) and endocannabinoid reuptake (in collaboration with industry and academic partners) are being addressed to target inflammatory diseases and neuropathic pain. Highly active and selective blockers of endocannabinoid reuptake are being developed to attenuate inflammation.

Gertsch and collaborators believe that therapeutically relevant membrane transporters should be systematically and intelligently screened to search for small organic compound allosteric modulators, and that structurally diverse natural products should be ideal candidates for tool and drug development. Given that drug discovery related issues become increasingly popular in academic settings it is important to integrate both basic research and applied biomedical sciences in this process. Gertsch is a Swiss MC member for the COST Action 0804 "Chemical Biology with Natural Products". In recognition to his work on natural product pharmacology he received the 2010 Dr. Willmar Schwabe award (Berlin, Germany) and for his work on cannabinoids (Gertsch et al. 2010, Br. J. Pharmacol. 160, 523) he obtained the Young Investigator Award Cannabinoids in Medicine 2010 (Jerusalem, Israel).

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