Identification of a Selective Inverse Agonist for the Orphan Nuclear Receptor Estrogen-Related Receptor α

2004 ◽  
Vol 47 (23) ◽  
pp. 5593-5596 ◽  
Author(s):  
Brett B. Busch ◽  
William C. Stevens, ◽  
Richard Martin ◽  
Peter Ordentlich ◽  
Sihong Zhou ◽  
...  
Keyword(s):  
Nuclear Receptor ◽  
Inverse Agonist ◽  
Orphan Nuclear Receptor ◽  
Estrogen Related Receptor

scholarly journals Orphan nuclear receptor oestrogen-related receptor γ (ERRγ) plays a key role in hepatic cannabinoid receptor type 1-mediated induction of CYP7A1 gene expression

2015 ◽  
Vol 470 (2) ◽  
pp. 181-193 ◽  
Author(s):  
Yaochen Zhang ◽  
Don-Kyu Kim ◽  
Ji-Min Lee ◽  
Seung Bum Park ◽  
Won-IL Jeong ◽  
...  
Keyword(s):  
Gene Expression ◽  
Bile Acid ◽  
Nuclear Receptor ◽  
Cannabinoid Receptor ◽  
Inverse Agonist ◽  
Receptor Type ◽  
Orphan Nuclear Receptor ◽  
Transcription Regulator ◽  
Estrogen Related Receptor

ERRγ is a novel transcription regulator of CYP7A1 (cholesterol 7α-hydroxylase). An ERRγ (Estrogen-related receptor γ) inverse agonist modulates bile acid homoeostasis via regulation of CYP7A1 gene expression.

scholarly journals Estrogen-related Receptor β (ERRβ) – Renaissance Receptor or Receptor Renaissance?

2016 ◽  
Vol 14 (1) ◽  
pp. nrs.14002 ◽  
Author(s):  
Shailaja D. Divekar ◽  
Deanna M. Tiek ◽  
Aileen Fernandez ◽  
Rebecca B. Riggins
Keyword(s):  
Alternative Splicing ◽  
Nuclear Receptor ◽  
Family Members ◽  
Structure And Function ◽  
The Other ◽  
Orphan Nuclear Receptor ◽  
Nuclear Receptor Superfamily ◽  
And Function ◽  
The Impact ◽  
Estrogen Related Receptor

Estrogen-related receptors (ERRs) are founding members of the orphan nuclear receptor (ONR) subgroup of the nuclear receptor superfamily. Twenty-seven years of study have yet to identify cognate ligands for the ERRs, though they have firmly placed ERRα (ESRRA) and ERRγ (ESRRG) at the intersection of cellular metabolism and oncogenesis. The pace of discovery for novel functions of ERRβ (ESRRB), however, has until recently been somewhat slower than that of its family members. ERRβ has also been largely ignored in summaries and perspectives of the ONR literature. Here, we provide an overview of established and emerging knowledge of ERRβ in mouse, man, and other species, highlighting unique aspects of ERRβ biology that set it apart from the other two estrogen-related receptors, with a focus on the impact of alternative splicing on the structure and function of this receptor.

scholarly journals Orphan Nuclear Receptor Estrogen-Related Receptor γ (ERRγ) Is Key Regulator of Hepatic Gluconeogenesis

2012 ◽  
Vol 287 (26) ◽  
pp. 21628-21639 ◽  
Author(s):  
Don-Kyu Kim ◽  
Dongryeol Ryu ◽  
Minseob Koh ◽  
Min-Woo Lee ◽  
Donghyun Lim ◽  
...  
Keyword(s):  
Nuclear Receptor ◽  
Orphan Nuclear Receptor ◽  
Hepatic Gluconeogenesis ◽  
Estrogen Related Receptor

scholarly journals Reduced Fat Mass in Mice Lacking Orphan Nuclear Receptor Estrogen-Related Receptor α

2003 ◽  
Vol 23 (22) ◽  
pp. 7947-7956 ◽  
Author(s):  
Jiangming Luo ◽  
Robert Sladek ◽  
Julie Carrier ◽  
Jo-Ann Bader ◽  
Denis Richard ◽  
...  
Keyword(s):  
Nuclear Receptor ◽  
Metabolic Regulation ◽  
Hormone Receptors ◽  
Target Genes ◽  
Serum Biochemistry ◽  
Orphan Nuclear Receptor ◽  
Steroid Synthesis ◽  
Fat Deposits ◽  
Estrogen Related Receptor

ABSTRACT The estrogen-related receptor α (ERRα) is an orphan member of the superfamily of nuclear hormone receptors expressed in tissues that preferentially metabolize fatty acids. Despite the molecular characterization of ERRα and identification of target genes, determination of its physiological function has been hampered by the lack of a natural ligand. To further understand the in vivo function of ERRα, we generated and analyzed Estrra-null (ERRα−/−) mutant mice. Here we show that ERRα−/− mice are viable, fertile and display no gross anatomical alterations, with the exception of reduced body weight and peripheral fat deposits. No significant changes in food consumption and energy expenditure or serum biochemistry parameters were observed in the mutant animals. However, the mutant animals are resistant to a high-fat diet-induced obesity. Importantly, DNA microarray analysis of gene expression in adipose tissue demonstrates altered regulation of several enzymes involved in lipid, eicosanoid, and steroid synthesis, suggesting that the loss of ERRα might interfere with other nuclear receptor signaling pathways. In addition, the microarray study shows alteration in the expression of genes regulating adipogenesis as well as energy metabolism. In agreement with these findings, metabolic studies showed reduced lipogenesis in adipose tissues. This study suggests that ERRα functions as a metabolic regulator and that the ERRα−/− mice provide a novel model for the investigation of metabolic regulation by nuclear receptors.

scholarly journals A Role for the Orphan Nuclear Receptor Estrogen-Related Receptor α in Endometrial Stromal Cell Decidualization and Expression of Genes Implicated in Energy Metabolism

Endocrinology ◽  
2010 ◽  
Vol 151 (9) ◽  
pp. 4594-4594 ◽  
Author(s):  
Vincent Bombail ◽  
Douglas Gibson ◽  
Frances Collins ◽  
Sheila MacPherson ◽  
Hilary O. D. Critchley ◽  
...  
Keyword(s):  
Energy Metabolism ◽  
Nuclear Receptor ◽  
Stromal Cell ◽  
Clinical Endocrinology ◽  
Orphan Nuclear Receptor ◽  
Endometrial Stromal Cell ◽  
Expression Of Genes ◽  
Estrogen Related Receptor

This article appears in The Journal of Clinical Endocrinology & Metabolism. 10.1210/jc.2010-0154

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