title: 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.
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Curt A
authors.initials: CA
authors.lastname: Dvorak
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Changlu
authors.initials: C
authors.lastname: Liu
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Jonathan
authors.initials: J
authors.lastname: Shelton
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Chester
authors.initials: C
authors.lastname: Kuei
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Steven W
authors.initials: SW
authors.lastname: Sutton
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.affiliation: Janssen Research & Development, LLC , San Diego, California 92121, United States.
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
keywords: FFA; GPR109a; GPR81; HCA1; agonist; flushing; lactate receptor; lipolysis; nicotinic acid receptor