Abstract
TRPM8 belongs to the TRPM Melastatin subfamily of Transient Receptor Potential (TRP) ion channels. Activated by cool temperatures and mimetic ligands, such as menthol and icilin, TRPM8 has been shown to play a role in thermoreception and is expressed in peripheral nerves. TRPM8 is also expressed in other tissues which are not exposed to temperature fluctuations, such as the prostate. The recent advancement of a TRPM8 agonist into the clinic for the treatment of prostate cancer suggests that the channel plays a role in some human pathologies. As more drug-like and selective agonists and antagonists of TRPM8 become available, in vivo pharmacology studies will complement already published knockout data to further our understanding of the role of TRPM8 in human disease.
Keywords: TRP, TRPM8, menthol, icilin, agonist, antagonist, ligand, Medicinal Chemistry, mimetic ligands, menthol and icilin, peripheral nerves, prostate cancer, knockout data, TRPM8 Protein, TRPM8 BIOLOGY
Current Topics in Medicinal Chemistry
Title: TRPM8 Biology and Medicinal Chemistry
Volume: 11 Issue: 17
Author(s): Jeff DeFalco, Matthew A.J. Duncton and Daniel Emerling
Affiliation:
Keywords: TRP, TRPM8, menthol, icilin, agonist, antagonist, ligand, Medicinal Chemistry, mimetic ligands, menthol and icilin, peripheral nerves, prostate cancer, knockout data, TRPM8 Protein, TRPM8 BIOLOGY
Abstract: TRPM8 belongs to the TRPM Melastatin subfamily of Transient Receptor Potential (TRP) ion channels. Activated by cool temperatures and mimetic ligands, such as menthol and icilin, TRPM8 has been shown to play a role in thermoreception and is expressed in peripheral nerves. TRPM8 is also expressed in other tissues which are not exposed to temperature fluctuations, such as the prostate. The recent advancement of a TRPM8 agonist into the clinic for the treatment of prostate cancer suggests that the channel plays a role in some human pathologies. As more drug-like and selective agonists and antagonists of TRPM8 become available, in vivo pharmacology studies will complement already published knockout data to further our understanding of the role of TRPM8 in human disease.
Export Options
About this article
Cite this article as:
DeFalco Jeff, A.J. Duncton Matthew and Emerling Daniel, TRPM8 Biology and Medicinal Chemistry, Current Topics in Medicinal Chemistry 2011; 11 (17) . https://dx.doi.org/10.2174/156802611796904933
DOI https://dx.doi.org/10.2174/156802611796904933 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Gastrointestinal Immune System and Brain Dialogue Implicated in Neuroinflammatory and Neurodegenerative Diseases
Current Molecular Medicine Editorial [Hot Topic: New Therapies in Prostate Cancer: Controlling Metastatic Disease and Preventing Oncogenesis (Executive Editor: B.F. Schwartz )]
Current Pharmaceutical Design Pharmacology of Cyclic Peptides: Vancomycin and Oxytocin as Paradigms
Protein & Peptide Letters The Ubiquitous Choline Transporter SLC44A1
Central Nervous System Agents in Medicinal Chemistry Therapeutic Potential of High Mobility Group Box-1 in Ischemic Injury and Tissue Regeneration
Current Vascular Pharmacology Patent Selections
Recent Patents on Anti-Infective Drug Discovery Cardiovascular Effects of Neuregulin-1/ErbB Signaling: Role in Vascular Signaling and Angiogenesis
Current Pharmaceutical Design Preparation and Evaluation of in vitro Self-assembling HSA Nanoparticles for Cabazitaxel
Anti-Cancer Agents in Medicinal Chemistry Functional Peptides and Small Molecules in Medicinal Chemistry-Part I
Current Topics in Medicinal Chemistry The Potential and Rationale for COX-2 Inhibitors in Lung Cancer
Anti-Cancer Agents in Medicinal Chemistry Highlights in Peptide Nanoparticle Carriers Intended to Oral Diseases
Current Topics in Medicinal Chemistry Nanoscale Formulations and Diagnostics With Their Recent Trends: A Major Focus of Future Nanotechnology
Current Pharmaceutical Design Anti-Angiogenesis in the Treatment of Genito-Urinary Cancers: Last Updates
Current Angiogenesis (Discontinued) The Vitamin D/CYP24A1 Story in Cancer
Anti-Cancer Agents in Medicinal Chemistry Imaging of Cyclooxygenase-2 (COX-2) Expression: Potential Use in Diagnosis and Drug Evaluation
Current Pharmaceutical Design Cardiovascular Tests: Use & Limits of Biochemical Markers - Therapeutic Measurements of ADMA Involved in Cardiovascular Disorders
Current Pharmaceutical Design Micro Arrays and Biochips: Applications and Potential in Genomics and Proteomics
Current Genomics Notch Signaling in Cardiovascular Disease and Calcification
Current Cardiology Reviews 6-Benzothiazolyl Ureas, Thioureas and Guanidines are Potent Inhibitors of ABAD/17β-HSD10 and Potential Drugs for Alzheimer"s Disease Treatment: Design, Synthesis and in vitro Evaluation
Medicinal Chemistry Studies on Structures and Functions of Kinases leading to Prostate Cancer and Their Inhibitors
Current Enzyme Inhibition