Abstract
TGR5 (also known as GPBAR1, M-BAR, BG37, hGPCR19, and AXOR 109) is a specific membrane Gprotein- coupled receptor (GPCR) of bile acids (BAs). It has recently become an attractive therapeutic target for the prevention and/or the treatment of obesity and its highly associated Type II diabetes and metabolic syndrome. It has also been implicated in many other inflammatory, cardiovascular, neurological, and hepatic diseases. This review briefly describes the biological rationale of TGR5 as an attractive therapeutic target and summarizes some recent efforts on the development of TGR5 modulators.
Keywords: G-protein-coupled receptor (GPCR), bile acids, TGR5, TGR5 modulators, obesity, Type II diabetes, metabolic syndrome
Current Topics in Medicinal Chemistry
Title: TGR5 as a Therapeutic Target for Treating Obesity
Volume: 10 Issue: 4
Author(s): Min Zhong
Affiliation:
Keywords: G-protein-coupled receptor (GPCR), bile acids, TGR5, TGR5 modulators, obesity, Type II diabetes, metabolic syndrome
Abstract: TGR5 (also known as GPBAR1, M-BAR, BG37, hGPCR19, and AXOR 109) is a specific membrane Gprotein- coupled receptor (GPCR) of bile acids (BAs). It has recently become an attractive therapeutic target for the prevention and/or the treatment of obesity and its highly associated Type II diabetes and metabolic syndrome. It has also been implicated in many other inflammatory, cardiovascular, neurological, and hepatic diseases. This review briefly describes the biological rationale of TGR5 as an attractive therapeutic target and summarizes some recent efforts on the development of TGR5 modulators.
Export Options
About this article
Cite this article as:
Zhong Min, TGR5 as a Therapeutic Target for Treating Obesity, Current Topics in Medicinal Chemistry 2010; 10 (4) . https://dx.doi.org/10.2174/156802610790980576
DOI https://dx.doi.org/10.2174/156802610790980576 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
The Mechanism of Carvedilol in Experimental Viral Myocarditis
Current Pharmaceutical Design Genetic Predisposition in NAFLD and NASH: Impact on Severity of Liver Disease and Response to Treatment
Current Pharmaceutical Design Effects of Sodium-Glucose Cotransporter-2 Inhibitors on Cardiac Structural and Electrical Remodeling: From Myocardial Cytology to Cardiodiabetology
Current Vascular Pharmacology Endothelin Receptor Antagonists: Another Potential Alternative for Cardiovascular Diseases
Current Drug Targets - Cardiovascular & Hematological Disorders Urocortin: Cardiovascular Actions and Therapeutic Implications
Letters in Drug Design & Discovery Epigenetic Modulation of Myocardial Angiogenic Balance: An Emerging Therapeutic Perspective for Adult Failing Heart
Current Angiogenesis (Discontinued) Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes
Current Medicinal Chemistry Oxidative/Nitrosative Stress and Immuno-inflammatory Pathways in Depression: Treatment Implications
Current Pharmaceutical Design Getting to the Heart of the Matter: Exploring Opportunities for Gene Therapy Treatment of Dystrophic Cardiomyopathy
Current Gene Therapy Treatment Approaches in Elderly Patients with Head and Neck Cancer
Anti-Cancer Agents in Medicinal Chemistry Lost in Translation: What is Limiting Cardiomyoplasty and Can Tissue Engineering Help?
Current Stem Cell Research & Therapy Pitavastatin and 4-Hydroxy-3-Methoxyacetophenone (HMAP) Reduce Cognitive Dysfunction in Vascular Dementia During Experimental Diabetes
Current Neurovascular Research Methods for Identifying Cardiovascular Agents: A Review
Recent Patents on Cardiovascular Drug Discovery Patent Selections:
Recent Patents on Cardiovascular Drug Discovery Chagas Disease Chemotherapy: What Do We Know So Far?
Current Pharmaceutical Design Myocardial Infarction in Systemic Lupus Erythematosus – the Sex-Specific Risk Profile
Current Pharmaceutical Design The Genetics of Small-Vessel Disease
Current Medicinal Chemistry Use of Contrast Echocardiography in Intensive Care and at the Emergency Room
Current Cardiology Reviews Transition of Care for Patients with Diabetes
Current Diabetes Reviews Using Extracellular Matrix-Derived Peptides to Alter the Microenvironment for Myocardial Repair
Current Vascular Pharmacology