Abstract
G protein-coupled receptors (GPCRs) constitute several membrane proteins that are turned on by hormones and neurotransmitters to trigger cellular signaling pathways. GPCRs have been targeted in the development of several drugs but the therapeutic potential of these proteins remains underutilized. Most drugs to date have targeted the class A, or the rhodopsin family of GPCRs, but recently the Class B, i.e., the secretin family of G protein receptors has been targeted for the treatment of metabolic diseases such as diabetes mellitus. Class B G protein-coupled receptors (GPCRs) have also been targeted for managing several clinical conditions such as diabetes mellitus, bone disorders, malignancies, neurodegeneration, cardiovascular diseases, neuropsychiatric disorders, etc. In this article, we review the medicinal chemistry and potential clinical role of targeting GPCRs with a special emphasis on cardiovascular pharmacology.
Keywords: Beta-arrestin, cardiovascular diseases, diabetes, G protein-coupled receptor, glucagon, heart failure, hypertrophy, ligand, rhodopsin, secretin.
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:G Protein-Coupled Receptors – Potential Roles in Clinical Pharmacology
Volume: 12 Issue: 1
Author(s): Megan Kypreos, Teesta Banerjee and Debabrata Mukherjee
Affiliation:
Keywords: Beta-arrestin, cardiovascular diseases, diabetes, G protein-coupled receptor, glucagon, heart failure, hypertrophy, ligand, rhodopsin, secretin.
Abstract: G protein-coupled receptors (GPCRs) constitute several membrane proteins that are turned on by hormones and neurotransmitters to trigger cellular signaling pathways. GPCRs have been targeted in the development of several drugs but the therapeutic potential of these proteins remains underutilized. Most drugs to date have targeted the class A, or the rhodopsin family of GPCRs, but recently the Class B, i.e., the secretin family of G protein receptors has been targeted for the treatment of metabolic diseases such as diabetes mellitus. Class B G protein-coupled receptors (GPCRs) have also been targeted for managing several clinical conditions such as diabetes mellitus, bone disorders, malignancies, neurodegeneration, cardiovascular diseases, neuropsychiatric disorders, etc. In this article, we review the medicinal chemistry and potential clinical role of targeting GPCRs with a special emphasis on cardiovascular pharmacology.
Export Options
About this article
Cite this article as:
Kypreos Megan, Banerjee Teesta and Mukherjee Debabrata, G Protein-Coupled Receptors – Potential Roles in Clinical Pharmacology, Cardiovascular & Hematological Agents in Medicinal Chemistry 2014; 12 (1) . https://dx.doi.org/10.2174/187152571201141201093751
DOI https://dx.doi.org/10.2174/187152571201141201093751 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |

- 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
Related Articles
-
Hyperglycemia and Perioperative Glucose Management
Current Pharmaceutical Design T Cell Replicative Senescence in Human Aging
Current Pharmaceutical Design Repurposing of Copper(II)-chelating Drugs for the Treatment of Neurodegenerative Diseases
Current Medicinal Chemistry Metabolic Regulation by the Hexosamine Biosynthesis/O-Linked N-Acetyl Glucosamine Pathway
Current Signal Transduction Therapy Review of Diabetic Polyneuropathy: Pathogenesis, Diagnosis and Management According to the Consensus of Egyptian Experts
Current Diabetes Reviews GABAergic Modulation in Diabetic Encephalopathy-Related Depression
Current Pharmaceutical Design Adipose Tissue in the Regulation of Inflammation
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Non-glycemic Adverse Effects of Insulin
Current Diabetes Reviews Established and In-trial GPCR Families in Clinical Trials: A Review for Target Selection
Current Drug Targets The Role of Sympathetic Nervous System in the Progression of Chronic Kidney Disease in the Era of Catheter Based Sympathetic Renal Denervation
Current Clinical Pharmacology Polyphenols in Disease: from Diet to Supplements
Current Pharmaceutical Biotechnology Nicotine Addiction and Coronary Artery Disease: Impact of Cessation Interventions
Current Pharmaceutical Design G-Lymphatic, Vascular and Immune Pathways for Aβ Clearance Cascade and Therapeutic Targets For Alzheimer’s Disease
Combinatorial Chemistry & High Throughput Screening Centenarian Offspring: A Model for Understanding Longevity
Current Vascular Pharmacology The Role of Parathyroid Hormone-Related Protein (PTHrP) in the Pathophysiology of Diabetes Mellitus
Mini-Reviews in Medicinal Chemistry Bitropic D3 Dopamine Receptor Selective Compounds s Potential Antipsychotics
Current Pharmaceutical Design Lack of Association between Genetic Polymorphism of Circadian Genes (PER2, PER3, CLOCK and OX2R) with Late Onset Depression and Alzheimer's Disease in a Sample of a Brazilian Population (Circadian Genes, Late-Onset Depression and Alzheimer's Disease)
Current Alzheimer Research Raloxifene and Cardiovascular Health: Its Relationship to Lipid and Glucose Metabolism, Hemostatic and Inflammation Factors and Cardiovascular Function in Postmenopausal Women
Current Pharmaceutical Design Pathophysiological Roles of Renin-Angiotensin System on Erythropoietic Action
Current Hypertension Reviews Impact of Endothelial NOS VNTR Variant on Susceptibility to Diabetic Neuropathy and Type 2 Diabetes Mellitus
Current Neurovascular Research