Characteristics of Nur77 and its ligands as potential anticancer compounds (Review).
Characteristics of Nur77 and its ligands as potential anticancer compounds (Review).
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Nur77 及其配体作为潜在抗癌化合物的特性
DOI：
10.3892/mmr.2018.9515
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发表时间：
2018-12
影响因子：
3.4
通讯作者：
Chen L
中科院分区：
文献类型：
--
作者：
Wu L;Chen L
核受体亚家族4组A成员1 （NR4A1，又称Nur77/TR3/NGFIB）是核受体超家族成员之一，作为早期应答基因表达，调控多个靶基因的表达。Nur77具有典型的核受体结构，包括n端结构域、DNA结合结构域和配体结合结构域。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首先被鉴定为孤儿受体，其内源性配体尚未鉴定；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方面具有有益作用。本文综述了Nur77的鉴定、结构、表达和定位、转录作用和非基因组功能，并总结了与Nur77相互作用的配体，包括细胞孢酮B、顺铂、TMPA、PDNPA、CCE9、THPN、z - liguslide、celastrol和双吲哚甲烷化合物，这些配体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.
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