Abstract
Transient Receptor Potential Melastatin-related 7 (TRPM7) is a non-selective cation channel fused with a functional kinase domain. Physiologically, TRPM7 channel is involved in magnesium homeostasis, cell survival and gastrulation. The channel part is responsible for calcium, magnesium, and metal trace entries. Cation current through TRPM7 channel is inhibited by both intracellular magnesium and magnesium complexed with nucleotides. In parallel, the kinase is able to phosphorylate cytoskeleton proteins like myosin chain regulating cell tension and motility. Moreover, TRPM7 kinase domain can be cleaved by caspase and participates to apoptosis signaling. Importantly, TRPM7 channel expression is aberrant in numerous cancers including breast, glioblastoma, nasopharynx, ovarian, and pancreatic. Moreover, TRPM7 high expression is an independent biomarker of poor outcome in breast cancer. Pharmacological modulation or silencing of TRPM7 strongly affects proliferation, adhesion, migration or invasion in cancer cell lines. Nevertheless, it is still not clear by which mechanism TRPM7 channels may disturb cancer cell hallmarks. In the present review, we will discuss the role of TRPM7 channels in malignancies. In particular, we will distinguish the role of cation signaling from kinase function in order to better understand how TRPM7 channels may play a central role in cancer progression. We will also discuss the recent advances in pharmacological blockers of TRPM7 and their potential use for cancer therapy.
Keywords: TRPM7, epithelial cancer, calcium, magnesium, kinase, pharmacological blockers.
Current Medicinal Chemistry
Title:Recent Advances in Oncogenic Roles of the TRPM7 Chanzyme
Volume: 23 Issue: 36
Author(s): Mathieu Gautier, Marianne Perrière, Michael Monet, Alison Vanlaeys, Irina Korichneva, Isabelle Dhennin-Duthille and Halima Ouadid-Ahidouch
Affiliation:
Keywords: TRPM7, epithelial cancer, calcium, magnesium, kinase, pharmacological blockers.
Abstract: Transient Receptor Potential Melastatin-related 7 (TRPM7) is a non-selective cation channel fused with a functional kinase domain. Physiologically, TRPM7 channel is involved in magnesium homeostasis, cell survival and gastrulation. The channel part is responsible for calcium, magnesium, and metal trace entries. Cation current through TRPM7 channel is inhibited by both intracellular magnesium and magnesium complexed with nucleotides. In parallel, the kinase is able to phosphorylate cytoskeleton proteins like myosin chain regulating cell tension and motility. Moreover, TRPM7 kinase domain can be cleaved by caspase and participates to apoptosis signaling. Importantly, TRPM7 channel expression is aberrant in numerous cancers including breast, glioblastoma, nasopharynx, ovarian, and pancreatic. Moreover, TRPM7 high expression is an independent biomarker of poor outcome in breast cancer. Pharmacological modulation or silencing of TRPM7 strongly affects proliferation, adhesion, migration or invasion in cancer cell lines. Nevertheless, it is still not clear by which mechanism TRPM7 channels may disturb cancer cell hallmarks. In the present review, we will discuss the role of TRPM7 channels in malignancies. In particular, we will distinguish the role of cation signaling from kinase function in order to better understand how TRPM7 channels may play a central role in cancer progression. We will also discuss the recent advances in pharmacological blockers of TRPM7 and their potential use for cancer therapy.
Export Options
About this article
Cite this article as:
Gautier Mathieu, Perrière Marianne, Monet Michael, Vanlaeys Alison, Korichneva Irina, Dhennin-Duthille Isabelle and Ouadid-Ahidouch Halima, Recent Advances in Oncogenic Roles of the TRPM7 Chanzyme, Current Medicinal Chemistry 2016; 23 (36) . https://dx.doi.org/10.2174/0929867323666160907162002
DOI https://dx.doi.org/10.2174/0929867323666160907162002 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the Treatment of Chronic Inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
Targeting Inhibitor of Apoptosis Proteins (IAPs) for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Novel Phospholipid-Based Labrasol Nanomicelles Loaded Flavonoids for Oral Delivery with Enhanced Penetration and Anti-Brain Tumor Efficiency
Current Drug Delivery Recent Developments in Targeted Therapies of the RAF-MEK and PI3KAKT Pathways in Cancer Treatment
Current Cancer Therapy Reviews Angiogenesis-Related Cytokines in Rheumatoid Arthritis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Brain MR Image Classification for Glioma Tumor detection using Deep Convolutional Neural Network Features
Current Medical Imaging Modulators of Acetylcholinesterase Activity: From Alzheimer's Disease to Anti-Cancer Drugs
Current Medicinal Chemistry MicroRNA Therapeutics: the Next Magic Bullet?
Mini-Reviews in Medicinal Chemistry Isoform-Selective PI3K Inhibitors for Various Diseases
Current Topics in Medicinal Chemistry Phosphoinositide 3-Kinases and Leukocyte Migration
Current Immunology Reviews (Discontinued) The Blood-Brain/Tumor Barriers: Challenges and Chances for Malignant Gliomas Targeted Drug Delivery
Current Pharmaceutical Biotechnology The Use of Cytokines and Chemokines in the Cancer Immunotherapy
Recent Patents on Anti-Cancer Drug Discovery Recent Advances on Glioblastoma Multiforme and Nano-drug Carriers: A Review
Current Medicinal Chemistry The Role of DNA Methylation in the Pathogenesis and Treatment of Cancer
Current Clinical Pharmacology Convection Enhanced Delivery of Macromolecules for Brain Tumors
Current Drug Discovery Technologies Magnetic Resonance Diffusion Tensor Imaging and Diffusion Tensor Tractography in the Evaluation of Congenital and Acquired Diseases of the Pediatric Visual System
Current Pediatric Reviews Molecular Response to Hypericin-Induced Photodamage
Current Medicinal Chemistry Tumor Vasculature Targeting Through NGR Peptide-Based Drug Delivery Systems
Current Pharmaceutical Biotechnology Immuno-Isolation in Oncology - A Mini-Review
Current Pharmaceutical Biotechnology Emerging Roles of Cysteine Cathepsins in Disease and their Potential as Drug Targets
Current Pharmaceutical Design Nanomedicine based on Nucleic Acids: Pharmacokinetic and Pharmacodynamic Perspectives
Current Pharmaceutical Biotechnology