Abstract
This article describes recent advances in the development and biological evaluation of small molecule mGluR4 positive allosteric modulators (PAMs), and, to a lesser extent, orthosteric agonists. Due to its expression in the basal ganglia, the Family 3 GPCR metabotropic glutamate receptor subtype 4 (mGluR4) has recently garnered a great deal of attention as a putative target for the treatment of Parkinsons disease and a variety of other CNS disorders. Until 2008, with the exception of the prototypical mGluR4 PAM ( – )-PHCCC, very few small molecule tools existed to probe the role of selective activation of mGluR4. This review will focus on the explosion of novel mGluR4 PAMs reported in the past year and the further preclinical validation of mGluR4 activation as a potentially groundbreaking treatment for Parkinsons disease.
Keywords: Metabotropic, mGluR4, Parkinson's disease, allosteric, positive allosteric modulator, dopamine, PHCCC, glutamate
Current Topics in Medicinal Chemistry
Title: Recent Progress in the Development of mGluR4 Positive Allosteric Modulators for the Treatment of Parkinsons Disease
Volume: 9 Issue: 10
Author(s): Craig W. Lindsley, Colleen M. Niswender, Darren W. Engers and Corey R. Hopkins
Affiliation:
Keywords: Metabotropic, mGluR4, Parkinson's disease, allosteric, positive allosteric modulator, dopamine, PHCCC, glutamate
Abstract: This article describes recent advances in the development and biological evaluation of small molecule mGluR4 positive allosteric modulators (PAMs), and, to a lesser extent, orthosteric agonists. Due to its expression in the basal ganglia, the Family 3 GPCR metabotropic glutamate receptor subtype 4 (mGluR4) has recently garnered a great deal of attention as a putative target for the treatment of Parkinsons disease and a variety of other CNS disorders. Until 2008, with the exception of the prototypical mGluR4 PAM ( – )-PHCCC, very few small molecule tools existed to probe the role of selective activation of mGluR4. This review will focus on the explosion of novel mGluR4 PAMs reported in the past year and the further preclinical validation of mGluR4 activation as a potentially groundbreaking treatment for Parkinsons disease.
Export Options
About this article
Cite this article as:
Lindsley W. Craig, Niswender M. Colleen, Engers W. Darren and Hopkins R. Corey, Recent Progress in the Development of mGluR4 Positive Allosteric Modulators for the Treatment of Parkinsons Disease, Current Topics in Medicinal Chemistry 2009; 9 (10) . https://dx.doi.org/10.2174/156802609789378272
DOI https://dx.doi.org/10.2174/156802609789378272 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Medicinal Chemistry Advancement in Life-Threatening Diseases
The current issue will highlight concise reports that specify ground-breaking insights, including the novel discovery of drug targets and their action mechanism or drugs of novel classes. These are projected to encourage medicinal chemistry future efforts to address the most challenging medical needs. The current issue highlights further efforts to ...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
-
Novel Therapies for Schizophrenia: Understanding the Glutamatergic Synapse and Potential Targets for Altering N-methyl-D-aspartate Neurotransmission
Recent Patents on CNS Drug Discovery (Discontinued) HPV as a Model for the Development of Prophylactic and Therapeutic Cancer Vaccines
Current Molecular Medicine Spatio-Temporal Fluctuations of Neural Dynamics in Mild Cognitive Impairment and Alzheimer’s Disease
Current Alzheimer Research Modeling and Simulation Approach to Support Dosing and Study Design Requirements for Treating HIV-Related Neuropsychiatric Disease with the NK1-R Antagonist Aprepitant
Current HIV Research The Case for Development of 11-Aza-artemisinins for Malaria
Current Medicinal Chemistry Quantitative Genetics in the Genomics Era
Current Genomics Pleiotropic Effects of Statins in Atherosclerotic Disease: Focus on the Antioxidant Activity of Atorvastatin
Current Topics in Medicinal Chemistry The Importance of Complying with Vaccination Protocols in Developed Countries: “Anti-Vax” Hysteria and the Spread of Severe Preventable Diseases
Current Medicinal Chemistry Deep Learning for Alzheimer’s Disease Classification using Texture Features
Current Medical Imaging Design, Synthesis and In Vitro Anti-microbial Evaluation of Ethylene/ Propylene-1H-1,2,3-Triazole-4-Methylene-tethered Isatin-coumarin Hybrids
Current Topics in Medicinal Chemistry Can FreeSurfer Compete with Manual Volumetric Measurements in Alzheimer’s Disease?
Current Alzheimer Research Modern Pathology: Protein Mis-Folding and Mis-Processing in Complex Disease
Current Protein & Peptide Science Apicoplast Import Protein Tic20 A Promising Therapeutic Molecular Target for Plasmodium falciparum: An In Silico Approach for Therapeutic Intervention
Infectious Disorders - Drug Targets Targeting Telomerase for Cancer Therapy
Current Cancer Therapy Reviews Breathing Generation and Potential Pharmacotherapeutic Approaches to Central Respiratory Disorders
Current Medicinal Chemistry BOOK REVIEW of “Craving for Ecstasy and Natural Highs:A Positive Approach to Mood Alteration”by Harvey B. Milkman & Stanley G. Sunderwirth
Current Drug Abuse Reviews Current Advances in Anti-Influenza Therapy
Current Medicinal Chemistry IL-6 Signaling and its Blockade with a Humanized Anti-Interleukin-6 Receptor Antibody in Rheumatoid Arthritis: Advent of a New and Innovative Therapeutic Drug, Tocilizumab
Current Rheumatology Reviews Preparation and Certification of Sulfamethoxazole Reference Material by Mass Balance Method and Differential Scanning Calorimetry
Current Analytical Chemistry Coinhibitory Molecule PD-1 as a Therapeutic Target in the Microenvironment of Multiple Myeloma
Current Cancer Drug Targets