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Modulators of TRPM7 and its potential as a drug target for brain tumours
Delphine Ji1, Andrea Fleig2, F David Horgen3
1Department of Surgery, Temerty Faculty of Medicine, University of Toronto, 1 King's College Circle, Toronto, Ontario, Canada M5S 1A8; Department of Physiology, Temerty Faculty of Medicine, University of Toronto, 1 King's College Circle, Toronto, Ontario, Canada M5S 1A8.
Abstract:
TRPM7 is a non-selective divalent cation channel with an alpha-kinase domain. Corresponding with its broad expression, TRPM7 has a role in a wide range of cell functions, including proliferation, migration, and survival. Growing evidence shows that TRPM7 is also aberrantly expressed in various cancers, including brain cancers. Because ion channels have widespread tissue distribution and result in extensive physiological consequences when dysfunctional, these proteins can be compelling drug targets. In fact, ion channels comprise the third-largest drug target type, following enzymes and receptors. Literature has shown that suppression of TRPM7 results in inhibition of migration, invasion, and proliferation in several human brain tumours. Therefore, TRPM7 presents a potential target for therapeutic brain tumour interventions. This article reviews current literature on TRPM7 as a potential drug target in the context of brain tumours and provides an overview of various selective and non-selective modulators of the channel relevant to pharmacology, oncology, and ion channel function.
Insights
Transient Receptor Potential Melastatin 7 (TRPM7) channel is implicated in brain tumor growth and survival. Suppressing TRPM7 inhibits cancer cell migration and proliferation, highlighting its potential as a therapeutic drug target.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Transient Receptor Potential Melastatin 7 (TRPM7) is a non-selective divalent cation channel with kinase activity.
- TRPM7 plays a crucial role in cell proliferation, migration, and survival.
- Aberrant TRPM7 expression is observed in various cancers, particularly brain tumors.
Purpose of the Study:
- To review current literature on TRPM7 as a potential drug target in brain tumors.
- To provide an overview of TRPM7 modulators relevant to pharmacology and oncology.
Main Methods:
- Literature review of studies investigating TRPM7 function and expression in brain cancers.
- Analysis of existing data on TRPM7 modulators (selective and non-selective).
Main Results:
- TRPM7 suppression inhibits migration, invasion, and proliferation in human brain tumors.
- Ion channels, including TRPM7, are significant drug targets due to their physiological roles.
Conclusions:
- TRPM7 represents a promising therapeutic target for brain tumor interventions.
- Understanding TRPM7 modulators is crucial for developing novel cancer therapies.
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