鉴定羟基苯甲酸为具有抗脂解作用的选择性乳酸受体（GPR81）激动剂。
Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.
作者信息
Dvorak Curt A, Liu Changlu, Shelton Jonathan, Kuei Chester, Sutton Steven W, Lovenberg Timothy W, Carruthers Nicholas I
机构信息
Janssen Research & Development, LLC , San Diego, California 92121, United States.
出版信息
ACS Med Chem Lett. 2012 Jun 11;3(8):637-9. doi: 10.1021/ml3000676. eCollection 2012 Aug 9.
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.
摘要
在对乳酸受体（GPR81）进行表征之后，一项重点筛选工作得到了3-羟基苯甲酸1，它是GPR81和GPR109a（烟酸受体）的弱激动剂。对结构相似的芳基羟基酸进行研究后，鉴定出了3-氯-5-羟基苯甲酸2，一种选择性GPR81激动剂，在肥胖小鼠模型中对脂肪分解表现出有利的体内效应。
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