College of Biological Science and Engineering, Fuzhou University, Fuzhou, Fujian 350108, P.R. China.
Mol Med Rep. 2018 Dec;18(6):4793-4801. doi: 10.3892/mmr.2018.9515. Epub 2018 Sep 27.
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.
核受体亚家族 4 组 A 成员 1（NR4A1；也称为 Nur77/TR3/NGFIB），是核受体超家族的成员，作为早期反应基因表达，调节多个靶基因的表达。Nur77 具有核受体的典型结构，包括 N 端结构域、DNA 结合域和配体结合域。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 最初被鉴定为孤儿受体，其内源性配体尚未确定；然而，越来越多的靶向 Nur77 的化合物已被报道在治疗癌症和其他疾病方面具有有益的作用。本文简要概述了 Nur77 的鉴定、结构、表达和定位、转录作用和非基因组功能，并总结了已证明与 Nur77 相互作用的配体，包括胞嘧啶酮 B、顺铂、TMPA、PDNPA、CCE9、THPN、Z- 榄香脂素、雷公藤红素和双吲哚甲烷化合物，它们可能潜在地用于治疗人类癌症。
