Modulators of TRPM7 and its potential as a drug target for brain tumours

Cell Calcium. 2022 Jan:101:102521. doi: 10.1016/j.ceca.2021.102521. Epub 2021 Dec 17.

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.

Keywords: TRPM7; brain tumor; brain tumour; drug development; drug target; gliomas; ion channels.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Brain Neoplasms* / drug therapy
  • Humans
  • Protein Serine-Threonine Kinases
  • TRPM Cation Channels* / antagonists & inhibitors

Substances

  • Antineoplastic Agents
  • TRPM Cation Channels
  • Protein Serine-Threonine Kinases
  • TRPM7 protein, human

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