Aebi_2024_Chimia.(Aarau)_78_499

Reference

Title : Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects - Aebi_2024_Chimia.(Aarau)_78_499
Author(s) : Aebi J , Atz K , Ametamey SM , Benz J , Blaising J , Butini S , Campiani G , Carreira EM , Collin L , De Lago E , Gazzi T , Gertsch J , Gobbi L , Guba W , Fernandez-Ruiz J , Fingerle J , Haider A , He Y , Heitman LH , Honer M , Hunziker D , Kuhn B , Maccarrone M , Marki HP , Martin RE , Mohr P , Mu L , Nazare M , Nippa DF , Oddi S , O'Hara F , Pacher P , Romero J , Rover S , Rufer AC , Schibli R , Schneider G , Stepan AF , Sykes DA , Ullmer C , van der Stelt M , Veprintsev DB , Wittwer MB , Grether U
Ref : Chimia (Aarau) , 78 :499 , 2024
Abstract :

The endocannabinoid system (ECS) is a critical regulatory network composed of endogenous cannabinoids (eCBs), their synthesizing and degrading enzymes, and associated receptors. It is integral to maintaining homeostasis and orchestrating key functions within the central nervous and immune systems. Given its therapeutic significance, we have launched a series of drug discovery endeavors aimed at ECS targets, including peroxisome proliferator-activated receptors (PPARs), cannabinoid receptors types 1 (CB1R) and 2 (CB2R), and monoacylglycerol lipase (MAGL), addressing a wide array of medical needs. The pursuit of new therapeutic agents has been enhanced by the creation of specialized labeled chemical probes, which aid in target localization, mechanistic studies, assay development, and the establishment of biomarkers for target engagement. By fusing medicinal chemistry with chemical biology in a comprehensive, translational end-to-end drug discovery strategy, we have expedited the development of novel therapeutics. Additionally, this strategy promises to foster highly productive partnerships between industry and academia, as will be illustrated through various examples.

PubMedSearch : Aebi_2024_Chimia.(Aarau)_78_499
PubMedID: 39221845

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Aebi J, Atz K, Ametamey SM, Benz J, Blaising J, Butini S, Campiani G, Carreira EM, Collin L, De Lago E, Gazzi T, Gertsch J, Gobbi L, Guba W, Fernandez-Ruiz J, Fingerle J, Haider A, He Y, Heitman LH, Honer M, Hunziker D, Kuhn B, Maccarrone M, Marki HP, Martin RE, Mohr P, Mu L, Nazare M, Nippa DF, Oddi S, O'Hara F, Pacher P, Romero J, Rover S, Rufer AC, Schibli R, Schneider G, Stepan AF, Sykes DA, Ullmer C, van der Stelt M, Veprintsev DB, Wittwer MB, Grether U (2024)
Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects
Chimia (Aarau) 78 :499

Aebi J, Atz K, Ametamey SM, Benz J, Blaising J, Butini S, Campiani G, Carreira EM, Collin L, De Lago E, Gazzi T, Gertsch J, Gobbi L, Guba W, Fernandez-Ruiz J, Fingerle J, Haider A, He Y, Heitman LH, Honer M, Hunziker D, Kuhn B, Maccarrone M, Marki HP, Martin RE, Mohr P, Mu L, Nazare M, Nippa DF, Oddi S, O'Hara F, Pacher P, Romero J, Rover S, Rufer AC, Schibli R, Schneider G, Stepan AF, Sykes DA, Ullmer C, van der Stelt M, Veprintsev DB, Wittwer MB, Grether U (2024)
Chimia (Aarau) 78 :499