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Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.


ABSTRACT: 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.

SUBMITTER: Dvorak CA 

PROVIDER: S-EPMC4025785 | biostudies-other | 2012 Aug

REPOSITORIES: biostudies-other

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Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.

Dvorak Curt A CA   Liu Changlu C   Shelton Jonathan J   Kuei Chester C   Sutton Steven W SW   Lovenberg Timothy W TW   Carruthers Nicholas I NI  

ACS medicinal chemistry letters 20120611 8


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. ...[more]

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