Transient receptor potential cation channel subfamily M member 4 (TRPM4)

Transient receptor potential cation channel subfamily M member 4 (TRPM4) is a tetrameric, calcium-activated, monovalent-selective cation channel that conducts mainly sodium and potassium ions but is impermeable to calcium[1][3][4]. It is widely expressed, including in cardiac tissue, immune cells, neurons, pancreatic β-cells, and smooth muscle. TRPM4 is activated by increased intracellular calcium and modulated by phosphoinositides and phosphorylation, enabling it to couple changes in cellular calcium to membrane depolarization without direct calcium influx. Mutations in TRPM4 are linked to cardiac conduction disorders, particularly progressive familial heart block. The channel plays roles in immunity, cardiac activity, insulin release, and smooth muscle function. Blockade can be achieved experimentally by various intracellular nucleotides and decavanadate[1][3]. There are currently no approved drugs specifically targeting TRPM4, but its disease associations and broad physiological roles make it a therapeutic target of significant interest.

Other names

TRPM4LTRPC4hTRPM4LTrpC-4LTrpC4FLJ20041Calcium-activated non-selective cation channel 1Long transient receptor potential channel 4Melastatin-4EKVP6PFHB1BTRPM4B

Channel blockade (by nucleotides and decavanadate: inhibition of monovalent cation flow); Modulation of channel activation (by calcium, PIP2, PKC phosphorylation, calmodulin)