Abstract
Family C of G-protein coupled receptors (GPCRs) from humans is constituted by eight metabotropic glutamate (mGlu1-8) receptors, two heterodimeric -aminobutyric acidB (GABAB) receptors, a calcium-sensing receptor (CaR), three taste (T1R) receptors, a promiscuous L- α-amino acid receptor (GPRC6A), and five orphan receptors. Aside from the orphan receptors, the family C GPCRs are characterised by a large amino-terminal domain, which bind the endogenous orthosteric agonists. Recently, a number of allosteric modulators binding to the seven transmembrane domains of the receptors have also been reported. Family C GPCRs regulate a number of important physiological functions and are thus intensively pursued as drug targets. So far, two drugs acting at family C receptors (the GABAB agonist baclofen and the positive allosteric CaR modulator cinacalcet) have been marketed. Cinacalcet is the first allosteric GPCR modulator to enter the market, which demonstrates that the therapeutic principle of allosteric modulation can also be extended to this important drug target class. In this review we outline the structure and function of family C GPCRs with particular focus on the ligand binding sites, and we present the most important pharmacological agents and the therapeutic prospects of the receptors.
Keywords: Metabotropic glutamate receptor, calcium-sensing receptor, γ-aminobutyric acidB receptor, GPRC6A
Current Drug Targets
Title: Structure, Pharmacology and Therapeutic Prospects of Family C G-Protein Coupled Receptors
Volume: 8 Issue: 1
Author(s): Hans Brauner-Osborne, Petrine Wellendorph and Anders A. Jensen
Affiliation:
Keywords: Metabotropic glutamate receptor, calcium-sensing receptor, γ-aminobutyric acidB receptor, GPRC6A
Abstract: Family C of G-protein coupled receptors (GPCRs) from humans is constituted by eight metabotropic glutamate (mGlu1-8) receptors, two heterodimeric -aminobutyric acidB (GABAB) receptors, a calcium-sensing receptor (CaR), three taste (T1R) receptors, a promiscuous L- α-amino acid receptor (GPRC6A), and five orphan receptors. Aside from the orphan receptors, the family C GPCRs are characterised by a large amino-terminal domain, which bind the endogenous orthosteric agonists. Recently, a number of allosteric modulators binding to the seven transmembrane domains of the receptors have also been reported. Family C GPCRs regulate a number of important physiological functions and are thus intensively pursued as drug targets. So far, two drugs acting at family C receptors (the GABAB agonist baclofen and the positive allosteric CaR modulator cinacalcet) have been marketed. Cinacalcet is the first allosteric GPCR modulator to enter the market, which demonstrates that the therapeutic principle of allosteric modulation can also be extended to this important drug target class. In this review we outline the structure and function of family C GPCRs with particular focus on the ligand binding sites, and we present the most important pharmacological agents and the therapeutic prospects of the receptors.
Export Options
About this article
Cite this article as:
Brauner-Osborne Hans, Wellendorph Petrine and Jensen A. Anders, Structure, Pharmacology and Therapeutic Prospects of Family C G-Protein Coupled Receptors, Current Drug Targets 2007; 8 (1) . https://dx.doi.org/10.2174/138945007779315614
DOI https://dx.doi.org/10.2174/138945007779315614 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...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
Related Articles
-
Cellular Communication in Bone Homeostasis and the Related Anti-osteoporotic Drug Development
Current Medicinal Chemistry Evaluation of Osteoporosis Risk Associated with Chronic Use of Morphine, Fentanyl and Tramadol in Adult Female Rats
Current Drug Safety Quantitative Proteomics with Isotope Dilution Analysis: Principles and Applications
Current Proteomics Roles of NHERF1/EBP50 in Cancer
Current Molecular Medicine Cancer as the Main Aging Factor for Humans: The Fundamental Role of 5-Methoxy-Tryptamine in Reversal of Cancer-Induced Aging Processes in Metabolic and Immune Reactions by Non-melatonin Pineal Hormones
Current Aging Science Patent Selections
Recent Patents on Drug Delivery & Formulation CRH Receptor Signalling: Potential Roles in Pathophysiology
Current Molecular Pharmacology Pharmacological Drug Delivery Strategies for Improved Therapeutic Effects: Recent Advances
Current Pharmaceutical Design Subject Index To Volume 8
Current Pharmaceutical Design The Role of Vitamin D in Gastrointestinal Diseases: Inflammation, Gastric Cancer, and Colorectal Cancer
Current Medicinal Chemistry Non-Analgesic Effects of Opioids: The Interaction of Opioids with Bone and Joints
Current Pharmaceutical Design Wound Healing Properties of Exosomes — A Review and Modelling of Combinatorial Analysis Strategies
Current Molecular Medicine Thyroid Ultrasound and Other Imaging Procedures in the Pediatric Age
Current Pediatric Reviews Management of Osteoporosis: Seeing the Future
Medicinal Chemistry Reviews - Online (Discontinued) Organic Cation Transporters: Physiology, Toxicology and Special Focus on Ethidium as a Novel Substrate
Current Drug Metabolism Inhibitors of the TGF-β Superfamily and their Clinical Applications
Mini-Reviews in Medicinal Chemistry Supertargeted Chemistry: Identifying Relationships Between Molecular Structures and their Sub-Cellular Distribution
Current Topics in Medicinal Chemistry Genetics of Congenital Heart Disease
Current Cardiology Reviews Medical Treatment of Malignancy-Associated Hypercalcemia
Current Medicinal Chemistry Recent Advances in the Membrane Receptor Initiated Vitamin D Signaling of Calcium and Phosphate Transport Across Intestinal and Kidney Epithelia
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued)