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
-
Vitamin D: Evolutionary, Physiological and Health Perspectives
Current Drug Targets Capsaicin Sensitive-Sensory Nerves and Blood Pressure Regulation
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Pomegranate Extract, A Prooxidant with Antiproliferative and Proapoptotic Activities Preferentially Towards Carcinoma Cells
Anti-Cancer Agents in Medicinal Chemistry Air Pollution Exposure and Blood Pressure: An Updated Review of the Literature
Current Pharmaceutical Design The Metabolic Syndrome and HIV Infection
Current Pharmaceutical Design Role of Statins in New-onset Diabetes Mellitus: The Underlying Cause, Mechanisms Involved, and Strategies to Combat
Current Drug Targets Dietary Fish Oil Concentrates Associated Health Benefits: A Recent Development of Cardiovascular Risk Reduction
Current Pharmaceutical Design Pleiotropic Effects of Cytokines on Acute Myocardial Infarction: G-CSF as A Novel Therapy for Acute Myocardial Infarction
Current Pharmaceutical Design 24-Hour Blood Pressure Control – A Predictor for Clinical Outcomes
Current Hypertension Reviews Can Serum Uric Acid Lowering Therapy Contribute to the Prevention or Treatment of Nonalcoholic Fatty Liver Disease?
Current Vascular Pharmacology Pharmacokinetic and Pharmacodynamic Variability: A Daunting Challenge in Drug Therapy
Current Drug Metabolism Having a Promising Efficacy on Type II Diabetes, It’s Definitely a Green Tea Time
Current Medicinal Chemistry The Metabolic Syndrome and Cardiovascular Risk
Current Diabetes Reviews Patent Selections:
Recent Patents on Cardiovascular Drug Discovery A Review of Cardiogenic Shock in Acute Myocardial Infarction
Current Cardiology Reviews Maternal Nutrition and Predisposition to Later Kidney Disease
Current Drug Targets Dysregulation of SIRT-1 Signaling in Multiple Sclerosis and Neuroimmune Disorders: A Systematic Review of SIRTUIN Activators as Potential Immunomodulators and their Influences on other Dysfunctions
Endocrine, Metabolic & Immune Disorders - Drug Targets Puerarin Stimulates Osteogenic Differentiation and Bone Formation Through the ERK1/2 and p38-MAPK Signaling Pathways
Current Molecular Medicine Oxidative Stress as a Regulator of Murine Atherosclerosis
Current Drug Targets Osteoblastic Responses to LPS, Glucose-oxidised LDL and Minocycline: Therapeutic Targets for Periodontal and Cardiometabolic Diseases
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery