Transient receptor potential melastatin-subfamily member 7 (TRPM7)

Transient receptor potential melastatin-subfamily member 7 (TRPM7) is a unique bifunctional protein that contains both a nonselective cation channel and a serine/threonine protein kinase (chanzyme) domain[1][2][3][8]. TRPM7 is a tetrameric transmembrane channel highly permeable to magnesium (Mg²⁺), zinc (Zn²⁺), and calcium (Ca²⁺) ions, and it is ubiquitously expressed across many tissues, playing an essential role in cellular Mg²⁺ homeostasis, development, proliferation, and signal transduction[1][2][3][4][7]. The channel is constitutively active and regulated by intracellular Mg²⁺ and Mg·ATP levels, along with phosphatidylinositol 4,5-bisphosphate (PIP₂)[4][5][7]. Its kinase domain can phosphorylate a variety of substrates, including nuclear histones, and participates in diverse signaling cascades important for cell viability and plasticity[1][8]. TRPM7 has been implicated as a therapeutic target in cancer, cardiovascular disease, neurodegeneration, and inflammation through its regulation of ionic balance and signaling pathways[1][2]. No selective small-molecule inhibitors of TRPM7 are clinically approved, but several molecules are used experimentally to probe its function. Safety concerns in targeting TRPM7 arise from its critical roles in electrolyte balance and embryonic development, amplifying the risk for broad physiological disruption if systemically blocked[1][2]. The commonly accepted abbreviation for this molecule is TRPM7. The canonical full name is transient receptor potential melastatin-subfamily member 7, following established protein nomenclature conventions.

Other names

TRPM7Chanzyme TRPM7Melastatin-related transient receptor potential channel 7Magnesium/nucleotide-regulated metal channel kinase

Inhibition of channel activity reduces cellular Mg²⁺ and Ca²⁺ influx Modulation affects downstream signaling by altering kinase activity