孤儿受体GPR139的研究进展

Research progress of orphan receptor GPR139

G蛋白偶联受体(G protein-coupled receptor, GPCR)是药物研发中最受关注的靶点。目前,临床上市药物中约34%是以GPCR为作用靶点。但是,至今仍有121个GPCR为孤儿受体。GPR139是主要存在于中枢神经系统的孤儿GPCR,在控制运动、动机和奖励的特定脑回路中高表达,与神经精神行为的调节相关。本文对GPR139的发现、组织表达、已报道的激动剂和拮抗剂、信号转导通路、与其他GPCR的相互作用及其生理功能等进行综述,为GPR139的深入研究寻找思路。

G protein coupled receptor(GPCR) is one of the most concerned drug targets in drug research and development. At present, 34% of currently marketed drugs target GPCR. However, there are presently 121 GPCRs which are still orphan receptors. GPR139 is an orphan GPCR that mainly exists in the central nervous system, and is highly expressed in selected brain circuits related to controlling movement, motivation and reward. GPR139 is associated with the regulation of neuropsychiatric behavior. This paper outlines the GPR139’s discovery, tissue expression, reported agonists and antagonists, signal transduction pathway, interaction with other GPCRs and its physiological functions, so as to find ideas for the further study of GPR139.