Review Article

Role of TRPM2 in brain tumours and potential as a drug target

Delphine Ji1,2, Zheng-wei Luo1,2, Andrea Ovcjak2, Rahmah Alanazi1,2, Mei-Hua Bao3, Zhong-Ping Feng2, Hong-Shuo Sun1,2,4,5
1 Department of Surgery, Temerty Faculty of Medicine, University of Toronto, Toronto, ON, Canada
2 Department of Physiology, Temerty Faculty of Medicine, University of Toronto, Toronto, ON, Canada
3 Science Research Center, Changsha Medical University, Changsha 410219, China
4 Department of Pharmacology and Toxicology, Temerty Faculty of Medicine, University of Toronto, Toronto, ON, Canada
5 Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, ON, Canada
Correspondence to: Zhong-Ping Feng:, Hong-Shuo Sun:,
DOI: 10.1038/s41401-021-00679-4
Received: 8 February 2021
Accepted: 7 April 2021
Advance online: 9 June 2021


Ion channels are ubiquitously expressed in almost all living cells, and are the third-largest category of drug targets, following enzymes and receptors. The transient receptor potential melastatin (TRPM) subfamily of ion channels are important to cell function and survival. Studies have shown upregulation of the TRPM family of ion channels in various brain tumours. Gliomas are the most prevalent form of primary malignant brain tumours with no effective treatment; thus, drug development is eagerly needed. TRPM2 is an essential ion channel for cell function and has important roles in oxidative stress and inflammation. In response to oxidative stress, ADP-ribose (ADPR) is produced, and in turn activates TRPM2 by binding to the NUDT9-H domain on the C-terminal. TRPM2 has been implicated in various cancers and is significantly upregulated in brain tumours. This article reviews the current understanding of TRPM2 in the context of brain tumours and overviews the effects of potential drug therapies targeting TRPM2 including hydrogen peroxide (H2O2), curcumin, docetaxel and selenium, paclitaxel and resveratrol, and botulinum toxin. It is long withstanding knowledge that gliomas are difficult to treat effectively, therefore investigating TRPM2 as a potential therapeutic target for brain tumours may be of considerable interest in the fields of ion channels and pharmacology.
Keywords: TRPM2; ion channels; gliomas; drug target; drug development

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