孤儿核受体Nur77的多功能性及其相关药物靶点作用机制的研究进展  

Research progress in orphan nuclear receptor Nur77 on the mechanisms of its multi-biological functions and drug targets

作　　者：周波 陈航姿[1] 吴乔[1] ZHOU Bo;CHEN Hangzi;WU Qiao(State Key Laboratory of Cellular Stress Biology,School of Life Sciences,Xiamen University,Xiamen 361102,China)

机构地区：[1]厦门大学生命科学学院,细胞应激生物学国家重点实验室,福建厦门361102

出　　处：《厦门大学学报（自然科学版）》2021年第2期277-289,共13页Journal of Xiamen University：Natural Science

基　　金：国家重点研发计划(2007CB914402,2011CB910802,2014CB910602,2016YFC1302403);国家自然科学基金(30630070,30810103905,31230019,U1405224,81730070,91853203,U1905206)。

摘　　要：核受体Nur77(也称TR3)是立早基因NR4A1编码的产物,在细胞增殖、分化、凋亡、自噬、炎症以及代谢等生命活动过程中发挥重要的调控作用.Nur77不仅作为转录因子调控下游靶基因的转录和表达,还能作为不依赖于转录的调节因子,通过蛋白相互作用以及改变亚细胞定位的方式发挥作用.Nur77的配体至今尚未在生物体内发现,因此它被称为孤儿核受体.然而,近年的研究已发现数个靶向Nur77并调控其功能的小分子药物.本文重点综述Nur77的多功能性、其体外激动剂和拮抗剂的筛选及其靶向调控的研究进展.Nuclear receptor Nur77(also known as TR3)is the protein product of NR4A1 gene,which plays an important role in regulating cell proliferation,differentiation,apoptosis,autophagy,inflammation and metabolism.As a transcription factor,Nur77 regulates the transcription and expression of downstream target genes,also acts as a regulator to regulate other proteins'functions through protein-protein interaction and subcellular localization changes.Although the physiological ligand of Nur77 has not been identified up to date,which attributed Nur77 to an orphan nuclear receptor,several Nur77 targeting compounds were identified.This review will focus on the research progress of multi-functions of Nur77,as well as the screening and targeting regulation of its agonists and antagonists.

关 键 词：孤儿核受体 Nur77 激动剂 拮抗剂 

分 类 号：Q291[生物学—细胞生物学]