Abstract
The family C seven transmembrane (7TM) receptors constitutes a small and especially well characterized subfamily of the large 7TM receptor superfamily. Approximately 50% of current prescription drugs target 7TM receptors, this biologically important family represents the largest class of drug-targets today. It is well established that family C 7TM receptors form homo- or hetero-dimers on the cell surface of living cells. The large extra-cellular domains (ECD) have been crystallized as a dimer in the presence and absence of agonist. Upon agonist binding, the dimeric ECD undergoes large conformational changes that lead to receptor activation. Despite extensive studies of the receptor transmembrane domain, several key features, including the exact organization of the complete receptor dimer, the sequence of events leading to receptor activation, and the functional significance of dimerization, have yet to be fully defined. This review presents the biochemical support for family C 7TM receptor dimerization and discusses its importance for receptor biosynthesis, surface expression, ligand binding and activation, since lessons learnt here may well be applicable to the whole superfamily of 7TM receptors.
Keywords: Family C, GPCR, dimerization, activation
Endocrine, Metabolic & Immune Disorders - Drug Targets
Title: Family C 7TM Receptor Dimerization and Activation
Volume: 6 Issue: 1
Author(s): Marie M. Bonde, Soren P. Sheikh and Jakob L. Hansen
Affiliation:
Keywords: Family C, GPCR, dimerization, activation
Abstract: The family C seven transmembrane (7TM) receptors constitutes a small and especially well characterized subfamily of the large 7TM receptor superfamily. Approximately 50% of current prescription drugs target 7TM receptors, this biologically important family represents the largest class of drug-targets today. It is well established that family C 7TM receptors form homo- or hetero-dimers on the cell surface of living cells. The large extra-cellular domains (ECD) have been crystallized as a dimer in the presence and absence of agonist. Upon agonist binding, the dimeric ECD undergoes large conformational changes that lead to receptor activation. Despite extensive studies of the receptor transmembrane domain, several key features, including the exact organization of the complete receptor dimer, the sequence of events leading to receptor activation, and the functional significance of dimerization, have yet to be fully defined. This review presents the biochemical support for family C 7TM receptor dimerization and discusses its importance for receptor biosynthesis, surface expression, ligand binding and activation, since lessons learnt here may well be applicable to the whole superfamily of 7TM receptors.
Export Options
About this article
Cite this article as:
Bonde M. Marie, Sheikh P. Soren and Hansen L. Jakob, Family C 7TM Receptor Dimerization and Activation, Endocrine, Metabolic & Immune Disorders - Drug Targets 2006; 6 (1) . https://dx.doi.org/10.2174/187153006776056594
DOI https://dx.doi.org/10.2174/187153006776056594 |
Print ISSN 1871-5303 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3873 |
- 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
-
Genetic Basis of Renal Mass in Rat Models
Current Hypertension Reviews Use of Clinically Available PPAR Agonists for Heart Failure; Do the Risks Outweigh the Potential Benefits?
Current Molecular Pharmacology Relationship Between Non-Genomic Actions of Estrogens and Insulin Resistace
Infectious Disorders - Drug Targets Ocular Neovascularization: Genomic Implications
Current Genomics Myocardial Infarction with and without ST-segment Elevation: a Contemporary Reappraisal of Similarities and Differences
Current Cardiology Reviews Atypical Herpetic Whitlow: A Diagnosis to Consider
Endocrine, Metabolic & Immune Disorders - Drug Targets Emerging Role of JNK in Insulin Resistance
Current Diabetes Reviews The Influence of Inflammatory Cytokines on the Proliferation and Osteoblastic Differentiation of MSCs
Current Stem Cell Research & Therapy Recent Advances in Glycomics and Glycogenetics
Current Topics in Medicinal Chemistry 1,4-Benzothiazines-A Biologically Attractive Scaffold
Mini-Reviews in Medicinal Chemistry A Review on Electrospun Nanofibers-based Electrochemical Sensor
Current Nanoscience ATP Binding Cassette Transporter A1 (ABCA1) Associated Proteins:Potential Drug Targets in the Metabolic Syndrome and Atherosclerotic Disease?
Current Pharmaceutical Biotechnology The Role of Melatonin in the Immuno-Neuro-Psychology of Mental Disorders
Recent Patents on CNS Drug Discovery (Discontinued) Stromal Cell-Derived Factor (SDF) 2 and the Endoplasmic Reticulum Stress Response of Trophoblast Cells in Gestational Diabetes Mellitus and <i>In vitro</i> Hyperglycaemic Condition
Current Vascular Pharmacology The Microbiota-Gut-Brain Axis in Neuropsychiatric Disorders: Pathophysiological Mechanisms and Novel Treatments
Current Neuropharmacology Leptin and the Cardiovascular System: A Review
Recent Patents on Cardiovascular Drug Discovery Discovery of JANUVIA <sup>TM</sup> (Sitagliptin), a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type2 Diabetes.
Current Topics in Medicinal Chemistry Identifying Risk Factors for Clinically Significant Diabetic Macula Edema in Patients with Type 2 Diabetes Mellitus
Current Diabetes Reviews Arterial Ischemic Stroke in Neonates and Children: Review and Current Issues
Current Pediatric Reviews Suramin: Clinical Uses and Structure-Activity Relationships
Mini-Reviews in Medicinal Chemistry