2-Phenoxy-nicotinamides are potent agonists at the bile acid receptor GPBAR1 (TGR5).

Authors :: Martin RE
Bissantz C
Gavelle O
Kuratli C
Dehmlow H
Richter HG
Obst Sander U
Erickson SD
Kim K
Pietranico-Cole SL
Alvarez-Sánchez R
Ullmer C
Source :: ChemMedChem [ChemMedChem] 2013 Apr; Vol. 8 (4), pp. 569-76. Date of Electronic Publication: 2012 Dec 07.
Publication Year :: 2013
Abstract: 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.<br /> (Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Subjects :: Binding Sites
Humans
Molecular Docking Simulation
Niacinamide metabolism
Protein Binding
Protein Structure, Tertiary
Quinolines chemistry
Receptors, G-Protein-Coupled metabolism
Structure-Activity Relationship
Niacinamide chemistry
Receptors, G-Protein-Coupled agonists

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