Abstract
Melanin concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy homeostasis. The MCH-1 receptor (MCH-R1) has been identified as a key target in MCH regulation, as small molecule antagonists of MCH-R1 have demonstrated activity in vivo. Herein, we chronicle our efforts to optimize a hit identified via high throughput screening of our proprietary compound library. Several challenges such as selectivity over other receptors, toxicity of a potential metabolite and determining receptor occupancy via a medium throughput assay will be reviewed.
Keywords: Melanin-concentrating hormone, MCH, MCH R1, MCH R1 antagonist, obesity
Current Topics in Medicinal Chemistry
Title: Melanin Concentrating Hormone Receptor Antagonists as Antiobesity Agents: From M2 to MCHR-1
Volume: 7 Issue: 15
Author(s): Mark D. McBriar
Affiliation:
Keywords: Melanin-concentrating hormone, MCH, MCH R1, MCH R1 antagonist, obesity
Abstract: Melanin concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy homeostasis. The MCH-1 receptor (MCH-R1) has been identified as a key target in MCH regulation, as small molecule antagonists of MCH-R1 have demonstrated activity in vivo. Herein, we chronicle our efforts to optimize a hit identified via high throughput screening of our proprietary compound library. Several challenges such as selectivity over other receptors, toxicity of a potential metabolite and determining receptor occupancy via a medium throughput assay will be reviewed.
Export Options
About this article
Cite this article as:
McBriar D. Mark, Melanin Concentrating Hormone Receptor Antagonists as Antiobesity Agents: From M2 to MCHR-1, Current Topics in Medicinal Chemistry 2007; 7 (15) . https://dx.doi.org/10.2174/156802607782194752
DOI https://dx.doi.org/10.2174/156802607782194752 |
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
-
Patent Selections:
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Recent Progress in Phosphoinositide 3-Kinases: Oncogenic Properties and Prognostic and Therapeutic Implications
Current Protein & Peptide Science Renal Tubular Acidosis
Current Pediatric Reviews Natural Animal Models of Neurodegenerative Protein Misfolding Diseases
Current Pharmaceutical Design Novel Anti-Inflammatory-Pro-Resolving Mediators and Their Receptors
Current Topics in Medicinal Chemistry Recent Highlights on Molecular Hybrids Potentially Useful in Central Nervous System Disorders
Mini-Reviews in Medicinal Chemistry Considering Autotaxin Inhibitors in Terms of 2D-QSAR and 3D-Mapping- Review and Evaluation
Current Medicinal Chemistry Is the Therapeutic Potential of Stem Cells for Myocardial Regeneration Limited by Proarrhythmic Effects?
Current Cardiology Reviews Role of Vascular Endothelial Growth Factor in Kidney Disease
Current Vascular Pharmacology Interplay of Carotenoids with Cigarette Smoking: Implications in Lung Cancer
Current Medicinal Chemistry Patent Annotations
Recent Patents on Anti-Infective Drug Discovery Review: New Anti-Cytokines for IBD: What is in the Pipeline?
Current Drug Targets The Tumor Suppressor Gene ARF as a Sensor of Oxidative Stress
Current Molecular Medicine Biology of Cox-2: An Application in Cancer Therapeutics
Current Drug Targets Pulmonary Rehabilitation as Evaluated by Clinical Trials: An Overview
Reviews on Recent Clinical Trials Application of Molecule-Ion Interactions Between Cyclodextrins and Ions in Inorganic Nanochemistry
Current Organic Chemistry Expanding our Understanding of Polyglutamine Disease Through Transgenic Mice
Current Genomics Cyclooxygenase-1 and -2 in the Different Stages of Alzheimers Disease Pathology
Current Pharmaceutical Design Glucocorticoids in Pregnancy
Current Pharmaceutical Biotechnology Subject Index To Volume 3
Current Alzheimer Research