TRPM2 channel properties, functions and therapeutic potentials

Expert Opin Ther Targets. 2010 Sep;14(9):973-88. doi: 10.1517/14728222.2010.510135.

Abstract

Importance of the field: Oxidative stress, through production of reactive oxygen species, triggers disturbance in intracellular calcium [Ca(2+)](i) homeostasis, which has been identified as an important causative factor in the pathogenesis of numerous inflammatory, cardiovascular and neurodegenerative diseases.

Areas covered in this review: Transient receptor potential melastatin 2 (TRPM2) protein forms a Ca(2+)-permeable cationic channel that is activated in response to oxidative stress and therefore acts as a cellular redox sensor. Research over the years has substantially advanced the knowledge of expression and functional properties of the TRPM2 channel, and particularly has accumulated compelling evidence for an important role for TRPM2 channel-mediated extracellular Ca(2+) influx in several physiological and pathophysiological functions exemplified by insulin release from pancreatic beta-cells, production of pro-inflammatory cytokines from immune cells, increased endothelial permeability, microglia activation and cell death. These findings suggest therapeutic potential of the TRPM2 channel as a drug target for combating oxidative-stress-related diseases.

What the reader will gain: The current state of knowledge with respect to the TRPM2 channel properties and the roles in oxidant stress signalling and functions.

Take home message: TRPM2 may be a novel therapeutic target for oxidative stress-related diseases.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Calcium / metabolism
  • Drug Delivery Systems*
  • Homeostasis
  • Humans
  • Oxidative Stress / drug effects*
  • Reactive Oxygen Species / metabolism
  • Signal Transduction / drug effects
  • TRPM Cation Channels / metabolism*

Substances

  • Reactive Oxygen Species
  • TRPM Cation Channels
  • TRPM2 protein, human
  • Calcium