Advances in function and ligands of transient receptor potential melastain 2 channels / 上海交通大学学报（医学版）

ABSTRACT

As nonselective cation channels, transient receptor potential melastain 2 (TRPM2) channels are widely distributed in the brain, mainly mediate the inflow of Na+ and Ca2+, leading to cell depolarization and the increasement of intracellular concentration of Ca2+, which are involved in many physiological and pathophysiological processes. Due to increased calcium concentration or oxidative stress, channel gating is induced by either direct or indirect formation of adenosine diphosphate ribose (ADPR) that binds to a NUDT9 homology domain (NUDT9-H) in the channel. There is no specific TRPM2 antagonist so far. Considering some pathological processes are mediated by TRPM2 channels, the study and discovery of specific TRPM2 blockers might contribute to the effective treatment of many related diseases.