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Transient receptor potential cation channel subfamily M member 2 (TRPM2) is a non-selective, calcium-permeable cation channel that belongs to the TRP superfamily of ion channels[5][8]. It is a homotetrameric protein activated by intracellular ADP-ribose, calcium, warm temperature, and oxidative stress, and is widely expressed, with particularly high levels in the brain, pancreas, and immune cells[1][2][5][8]. TRPM2 mediates calcium influx in response to oxidative and metabolic stress, playing roles in immune response, thermosensation, cell death pathways, and metabolic regulation (notably insulin secretion). Dysregulation of TRPM2 is associated with cancer cell viability, neurodegenerative diseases like Alzheimer’s, inflammatory and metabolic diseases, and may influence psychiatric disorders[5][2]. While considered a promising therapeutic target, no selective drugs are in clinical use due to challenges in achieving specificity and the widespread physiological functions of the channel.
Ligand-gated ion channel blockade (inhibition of channel opening); Modulation of ADP-ribose binding and hydrolysis; Regulation of calcium influx following oxidative stress
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