Abstract
Rev-erbs are members of the nuclear receptor (NR) transcription factor superfamily and are widely expressed, but are most prevalent in liver, adipose tissue, skeletal muscle and brain. Rev-erbs are key regulators of the circadian rhythm and are expressed in a circadian manner. The discovery that Rev-erbs are ligand-regulated receptors, whose repressive activity is regulated by the endogenous porphyrin ligand, heme, as well as the recent report of the first synthetic Rev-erb ligand, GSK4112/SR6452, suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases. Here, we review the work leading to the discovery that Rev-erbs are indeed ligand-regulated and the role that both natural and synthetic Rev-erb ligands have on adipogenesis.
Keywords: Nuclear receptor, heme, GSK4112, SR6452, adipogenesis, metabolism, diabetes, obesity
Current Pharmaceutical Design
Title: A Role for Rev-erbα Ligands in the Regulation of Adipogenesis
Volume: 17 Issue: 4
Author(s): Douglas J. Kojetin and Thomas P. Burris
Affiliation:
Keywords: Nuclear receptor, heme, GSK4112, SR6452, adipogenesis, metabolism, diabetes, obesity
Abstract: Rev-erbs are members of the nuclear receptor (NR) transcription factor superfamily and are widely expressed, but are most prevalent in liver, adipose tissue, skeletal muscle and brain. Rev-erbs are key regulators of the circadian rhythm and are expressed in a circadian manner. The discovery that Rev-erbs are ligand-regulated receptors, whose repressive activity is regulated by the endogenous porphyrin ligand, heme, as well as the recent report of the first synthetic Rev-erb ligand, GSK4112/SR6452, suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases. Here, we review the work leading to the discovery that Rev-erbs are indeed ligand-regulated and the role that both natural and synthetic Rev-erb ligands have on adipogenesis.
Export Options
About this article
Cite this article as:
J. Kojetin Douglas and P. Burris Thomas, A Role for Rev-erbα Ligands in the Regulation of Adipogenesis, Current Pharmaceutical Design 2011; 17 (4) . https://dx.doi.org/10.2174/138161211795164211
DOI https://dx.doi.org/10.2174/138161211795164211 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Stress Myocardial Perfusion Imaging in the Emergency Department - New Techniques for Speed and Diagnostic Accuracy
Current Cardiology Reviews Angiotensin 1-7 Promotes Cardiac Angiogenesis Following Infarction
Current Vascular Pharmacology Cardiac Rehabilitation Outcome Following Percutaneous Coronary Intervention Compared to Cardiac Surgery
Recent Patents on Cardiovascular Drug Discovery Cardiovascular Pharmacogenetics of Antihypertensive and Lipid- Lowering Therapies
Current Molecular Medicine Transthyretin Cardiac Amyloidosis and Aortic Stenosis: Connection and Therapeutic Implications
Current Cardiology Reviews Pleiotropic Effects of Rimonabant: Clinical Implications
Current Pharmaceutical Design Innate Immunity and the Heart
Current Pharmaceutical Design Enhanced Antioxidant and Protective Activities on Retinal Ganglion Cells of Carotenoids-Overexpressing Transgenic Carrot
Current Drug Targets The Use of Exercise Echocardiography in the Evaluation of Mitral Regurgitation
Current Cardiology Reviews Life Threatening and Fatal Contrast Media Reactions: Pathomechanisms, Diagnosis, Prevention and Drug Management
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cardiovascular disease management through restrained inflammatory responses
Current Pharmaceutical Design Recent Advances on the Roles of NO in Cancer and Chronic Inflammatory Disorders
Current Medicinal Chemistry Ivabradine: A Current Overview
Current Clinical Pharmacology Novel Non-Steroidal Anti-Inflammatory Drugs: What we have Learned from Animal Studies
Current Drug Targets - Inflammation & Allergy An Overview of Innovations in Analysis and Beneficial Health Effects of Wine Polyphenols
Mini-Reviews in Medicinal Chemistry Novel Carriers for Coenzyme Q10 Delivery
Current Drug Delivery The Anti-Inflammatory and Pharmacological Actions of Oleocanthal, a Phenolic Contained in Extra Virgin Olive Oil
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Recent Patents in siRNA Delivery Employing Nanoparticles as Delivery Vectors
Recent Patents on DNA & Gene Sequences Headspace Analyses in Valuable and Functional Foods: Application of SPME in the Quality Control and Characterization of Olive Oils
Current Analytical Chemistry Torsades de Pointes in Patients with Polymyalgia Rheumatica
Current Pharmaceutical Design