scholarly journals Estrogen-Related Receptor Alpha: An Under-Appreciated Potential Target for the Treatment of Metabolic Diseases

2020 ◽  
Vol 21 (5) ◽  
pp. 1645 ◽  
Author(s):  
Madhulika Tripathi ◽  
Paul Michael Yen ◽  
Brijesh Kumar Singh

The estrogen-related receptor alpha (ESRRA) is an orphan nuclear receptor (NR) that significantly influences cellular metabolism. ESRRA is predominantly expressed in metabolically-active tissues and regulates the transcription of metabolic genes, including those involved in mitochondrial turnover and autophagy. Although ESRRA activity is well-characterized in several types of cancer, recent reports suggest that it also has an important role in metabolic diseases. This minireview focuses on the regulation of cellular metabolism and function by ESRRA and its potential as a target for the treatment of metabolic disorders.

2016 ◽  
Vol 14 (1) ◽  
pp. nrs.14002 ◽  
Author(s):  
Shailaja D. Divekar ◽  
Deanna M. Tiek ◽  
Aileen Fernandez ◽  
Rebecca B. Riggins

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.


2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Lei Zhang ◽  
Qun Wang ◽  
Wen Liu ◽  
Fangyan Liu ◽  
Ailing Ji ◽  
...  

Orphan nuclear receptor 4A1 (NR4A1) is a transcriptional factor of the nuclear orphan receptor (NR4A) superfamily that has sparked interest across different research fields in recent years. Several studies have demonstrated that ligand-independent NR4A1 is an immediate-early response gene and the protein product is rapidly induced by a variety of stimuli. Hyperfunction or dysfunction of NR4A1 is implicated in various metabolic processes, including carbohydrate metabolism, lipid metabolism, and energy balance, in major metabolic tissues, such as liver, skeletal muscle, pancreatic tissues, and adipose tissues. No endogenous ligands for NR4A1 have been identified, but numerous compounds that bind and activate or inactivate nuclear NR4A1 or induce cytoplasmic localization of NR4A1 have been identified. This review summarizes recent advances in our understanding of the molecular biology and physiological functions of NR4A1. And we focus on the physiological functions of NR4A1 receptor to the development of the metabolic diseases, with a special focus on the impact on carbohydrate and lipid metabolism in skeletal muscle, liver, adipose tissue, and islet.


2015 ◽  
Vol 470 (2) ◽  
pp. 181-193 ◽  
Author(s):  
Yaochen Zhang ◽  
Don-Kyu Kim ◽  
Ji-Min Lee ◽  
Seung Bum Park ◽  
Won-IL Jeong ◽  
...  

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.


2019 ◽  
Vol 99 (12) ◽  
pp. 1835-1849 ◽  
Author(s):  
Ramy K. A. Sayed ◽  
Doaa M. Mokhtar ◽  
Marisol Fernández-Ortiz ◽  
Germaine Escames ◽  
Darío Acuña-Castroviejo

2012 ◽  
Vol 287 (26) ◽  
pp. 21628-21639 ◽  
Author(s):  
Don-Kyu Kim ◽  
Dongryeol Ryu ◽  
Minseob Koh ◽  
Min-Woo Lee ◽  
Donghyun Lim ◽  
...  

Biochimie ◽  
2005 ◽  
Vol 87 (1) ◽  
pp. 21-25 ◽  
Author(s):  
S Laitinen ◽  
C Fontaine ◽  
JC Fruchart ◽  
B Staels

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