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2‐Phenoxy‐nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)
Author(s) -
Martin Rainer E.,
Bissantz Caterina,
Gavelle Olivier,
Kuratli Christoph,
Dehmlow Henrietta,
Richter Hans G. F.,
Obst Sander Ulrike,
Erickson Shawn D.,
Kim Kyungjin,
PietranicoCole Sherrie Lynn,
AlvarezSánchez Rubén,
Ullmer Christoph
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200474
Subject(s) - computational biology , receptor , agonist , chemistry , biochemistry , computer science , biology
Potency with potential: 2‐Phenoxy‐ nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure–activity relationship studies supported by homology modeling and docking resulted in the identification of optimized GPBAR1 agonists, potent against both human and mouse receptors, endowed with favorable physicochemical properties and good metabolic stability.