核受体亚家族4组A成员1(NR4A1;也称为Nur77/TR3/NGFIB),核受体超家族的成员,表达为早期反应基因,调控多个靶基因的表达。Nur77具有核受体的典型结构,包括一个N端域,DNA结合域,和一个配体结合域。Nur77的表达和定位与其在细胞增殖和凋亡中的作用密切相关。Nur77最初被确定为孤儿受体,其内源性配体尚未确定;然而,据报道,越来越多的靶向Nur77的化合物在治疗癌症和其他疾病中具有有益作用。这篇综述简要概述了鉴定,结构,表达和本地化,Nur77的转录作用和非基因组功能,并总结了已显示与Nur77相互作用的配体,包括细胞孢素B,顺铂,TMPA,PDNPA,CCE9,THPN,Z-齐斯利特,celastrol和双吲哚甲烷化合物,可能用于治疗人类癌症。
Nuclear receptor subfamily 4 group A member 1 (NR4A1; also termed Nur77/TR3/NGFIB), a member of the nuclear receptor superfamily, is expressed as an early response gene to regulate the expression of multiple target genes. Nur77 has the typical structure of a nuclear receptor, including an N‑terminal domain, a DNA binding domain, and a ligand‑binding domain. The expression and localization of Nur77 are closely associated with its roles in cell proliferation and apoptosis. Nur77 was first identified as an orphan receptor, the endogenous ligand of which has not yet been identified; however, an increasing number of compounds targeting Nur77 have been reported to have beneficial effects in the treatment of cancer and other diseases. This
review provides a brief overview of the identification, structure, expression and localization, transcriptional role and non‑genomic function of Nur77, and summarizes the ligands that have been shown to interact with Nur77, including cytosporone B, cisplatin, TMPA, PDNPA, CCE9, THPN, Z‑ligustilide, celastrol and bisindole methane compounds, which may potentially be used to treat cancer in humans.