REV-ERBα
REV-ERBα (nuclear receptor subfamily 1 group D member 1, NR1D1) is a heme-binding nuclear receptor that functions as a transcriptional regulator within the circadian clock machinery[1][2]. REV-ERBα represses transcription by recruiting corepressor complexes containing nuclear receptor corepressor (NCoR) and histone deacetylase 3 (HDAC3) to REV-ERB response elements in target genes[2][3]. Mechanistically, REV-ERBα regulates circadian gene expression through feedback control of core clock components, including repression of Bmal1 transcription[1][3]. REV-ERBα connects circadian regulation with metabolic pathways by controlling genes involved in lipid metabolism, glucose homeostasis, mitochondrial function, and inflammatory responses[2][4]. In experimental models, REV-ERBα disruption alters circadian rhythms and affects metabolic phenotypes, including changes in energy balance and inflammatory regulation[4][5]. Compared with the related isoform REV-ERBβ (NR1D2), REV-ERBα shares conserved DNA-binding and ligand-binding domains but exhibits distinct tissue expression patterns and physiological contributions within circadian regulation[6]. REV-ERBα differs from many nuclear receptors because it functions primarily as a transcriptional repressor rather than a ligand-activated transcriptional activator[1][2]. For experimental applications, REV-ERBα activity is studied using genetic deletion models, reporter assays, chromatin immunoprecipitation, and pharmacological modulation approaches[3][5]. Synthetic REV-ERB agonists, including SR9009 and related compounds, have been used to investigate circadian regulation, metabolism, and inflammatory pathways in experimental models[7].
References:
- [1]. Raghuram S, et al. Identification of heme as the ligand for the orphan nuclear receptors REV-ERBα and REV-ERBβ. Nature Structural Molecular Biology. 2007;14(12):1207-1213. [Content Brief]
- [2]. Duez H, et al. The nuclear receptors Rev-erbs and RORs integrate circadian rhythms and metabolism. Diabetes, Vascular Disease Research. 2008;5(2):82-88. [Content Brief]
- [3]. Yin L, et al. The orphan nuclear receptor Rev-erbα recruits the N-CoR/histone deacetylase 3 corepressor to regulate the circadian Bmal1 gene. Molecular Endocrinology. 2005;19(6):1452-1459. [Content Brief]
- [4]. Cho H, et al. Regulation of circadian behaviour and metabolism by REV-ERBα and REV-ERBβ. Nature. 2012;485(7396):123-127. [Content Brief]
- [5]. Bugge A, et al. Rev-erbα and Rev-erbβ coordinately protect the circadian clock and normal metabolic function. Genes Development. 2012;26(7):657-667. [Content Brief]
- [6]. Preitner N, et al. The orphan nuclear receptor REV-ERBα controls circadian transcription within the positive limb of the mammalian circadian oscillator. Cell. 2002;110(2):251-260. [Content Brief]
- [7]. Solt LA, et al. Regulation of circadian and metabolic behavior by REV-ERB agonists. Nature. 2012;485(7396):62-68. [Content Brief]
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REV-ERBα Related Products (2)
Related Products (2)
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CM002
0 ImagesCat. No.: HY-184895CM002 is a circadian clock activator. CM002 inhibits the lineage commitment and terminal differentiation of preadipocytes by activating the circadian clock, thereby blocking the adipogenesis process driven by Wnt signaling-mediated transcriptional induction. CM002 attenuates lipid storage in a clock-dependent manner via inhibition of the lipogenic program in mature adipocytes. CM002 enhances circadian clock output across various adipose depots in both lean and obese mice through BMAL1/CLOCK-dependent metabolic reprogramming, inhibits adipocyte development and hypertrophy, and improves insulin sensitivity. CM002 can be used in research on obesity and type 2 diabetes.
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(R)-SR-29065
0 ImagesCat. No.: HY-156458ACAS No.: 2756883-91-5(R)-SR-29065 is a selective REV-ERBα inhibitor with a IC50 of 10 nM. (R)-SR-29065 is applicable to research related to autoimmune diseases.
