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Characteristics of Nur77 and Its Ligands as Potential Anticancer Compounds (Review)

Lingjuan Wu, Liqun Chen

Mol Med Rep. 2018 Dec;18(6):4793-4801.

PMID: 30272297

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP100079263 THPN THPN 100079-26-3 Price
AP321661625 Cytosporone B Cytosporone B 321661-62-5 Price
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