Identification of hydroxybenzoic acids as selective lactate receptor (GPR81) agonists with antilipolytic effects
CA Dvorak, C Liu, J Shelton, C Kuei… - ACS medicinal …, 2012 - ACS Publications
CA Dvorak, C Liu, J Shelton, C Kuei, SW Sutton, TW Lovenberg, NI Carruthers
ACS medicinal chemistry letters, 2012•ACS PublicationsFollowing the characterization of the lactate receptor (GPR81), a focused screening effort
afforded 3-hydroxybenzoic acid 1 as a weak agonist of both GPR81 and GPR109a (niacin
receptor). An examination of structurally similar arylhydroxy acids led to the identification of 3-
chloro-5-hydroxybenzoic acid 2, a selective GPR81 agonist that exhibited favorable in vivo
effects on lipolysis in a mouse model of obesity.
afforded 3-hydroxybenzoic acid 1 as a weak agonist of both GPR81 and GPR109a (niacin
receptor). An examination of structurally similar arylhydroxy acids led to the identification of 3-
chloro-5-hydroxybenzoic acid 2, a selective GPR81 agonist that exhibited favorable in vivo
effects on lipolysis in a mouse model of obesity.
Following the characterization of the lactate receptor (GPR81), a focused screening effort afforded 3-hydroxybenzoic acid 1 as a weak agonist of both GPR81 and GPR109a (niacin receptor). An examination of structurally similar arylhydroxy acids led to the identification of 3-chloro-5-hydroxybenzoic acid 2, a selective GPR81 agonist that exhibited favorable in vivo effects on lipolysis in a mouse model of obesity.
ACS Publications