Abstract
Class C G protein-coupled receptors encompass a range of promising therapeutic targets for a variety of diseases, yet to date only two members of this sub-family of GPCRs have been drugged. Recent advances in structural biology have revealed the X-ray crystallographic structures of allosteric ligands bound to two Class C metabotropic glutamate (mGlu) receptors, mGlu1 and mGlu5. Herein, we review how this information can be leveraged to help understand some of the historical challenges of mGlu receptor allosteric modulator drug discovery, and discuss how the structural enablement can be prospectively used for structurebased drug discovery approaches across Class C GPCR targets in general.
Keywords: Allosteric, CNS, Crystallography, Glutamate, GPCR, Modulator.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Potential for the Rational Design of Allosteric Modulators of Class C GPCRs
Volume: 17 Issue: 1
Author(s): John A. Christopher, Andrew S. Doré and Benjamin G. Tehan
Affiliation:
Keywords: Allosteric, CNS, Crystallography, Glutamate, GPCR, Modulator.
Abstract: Class C G protein-coupled receptors encompass a range of promising therapeutic targets for a variety of diseases, yet to date only two members of this sub-family of GPCRs have been drugged. Recent advances in structural biology have revealed the X-ray crystallographic structures of allosteric ligands bound to two Class C metabotropic glutamate (mGlu) receptors, mGlu1 and mGlu5. Herein, we review how this information can be leveraged to help understand some of the historical challenges of mGlu receptor allosteric modulator drug discovery, and discuss how the structural enablement can be prospectively used for structurebased drug discovery approaches across Class C GPCR targets in general.
Export Options
About this article
Cite this article as:
Christopher A. John, Doré S. Andrew and Tehan G. Benjamin, Potential for the Rational Design of Allosteric Modulators of Class C GPCRs, Current Topics in Medicinal Chemistry 2017; 17 (1) . https://dx.doi.org/10.2174/1568026616666160719165922
DOI https://dx.doi.org/10.2174/1568026616666160719165922 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Preface [Hot topic: Potential Therapeutic Agents for Parkinsons Disease (Executive Editor: Masato Asanuma)]
Current Pharmaceutical Design Protein-C Reactive as Biomarker Predictor of Schizophrenia Phases of Illness? A Systematic Review
Current Neuropharmacology Regression to the Mean: Implications for Clinical Trials of Psychotropic Agents in Dementia
Current Alzheimer Research Nitric Oxide in Health and Disease from the Point of View of the Otorhinolaryngologist
Current Pharmaceutical Design Pharmacological Applications of Antioxidants: Lights and Shadows
Current Drug Targets Animal Models for Parkinson's Disease
CNS & Neurological Disorders - Drug Targets Non-Analgesic Effects of Opioids: Interactions Between Opioids and Other Drugs
Current Pharmaceutical Design Antipsychotic Induced Dopamine Supersensitivity Psychosis: A Comprehensive Review
Current Neuropharmacology Applications of Lentiviral Vectors for Biology and Gene Therapy of Neurological Disorders
Current Gene Therapy GDNF Family Ligands: A Potential Future for Parkinson's Disease Therapy
CNS & Neurological Disorders - Drug Targets Advances in the Physiology of GPR55 in the Central Nervous System
Current Neuropharmacology Therapeutic Hypothermia in Brain Injuries and Related Diseases
Recent Patents on Inflammation & Allergy Drug Discovery The Role of Neurogenesis in Neurodegenerative Diseases and its Implications for Therapeutic Development
CNS & Neurological Disorders - Drug Targets Blockers of Voltage-Gated Sodium Channels for the Treatment of Central Nervous System Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Targeting the Progression of Parkinsons Disease
Current Neuropharmacology Serotonin Control of Dopaminergic Neurotransmission: Focus on 5-HT2 Receptors
Current Neuropharmacology Melatonin Receptor Agonists: SAR and Applications to the Treatment of Sleep-Wake Disorders
Current Topics in Medicinal Chemistry GABAB Receptors as Potential Therapeutic Targets
Current Drug Targets - CNS & Neurological Disorders The Rabbit Syndrome: State of the Art
Current Clinical Pharmacology The Chemical Biology of Immunophilin Ligands
Current Medicinal Chemistry