【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.更多还原

【Abstract】 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.更多还原