Transient receptor potential melastatin-related cation channel subfamily M member 7 (TRPM7)

Transient receptor potential melastatin-related cation channel subfamily M member 7 (TRPM7) is a bifunctional transmembrane protein combining a non-selective cation channel and an intrinsic serine/threonine protein kinase domain. It forms a homo-tetrameric complex, enabling passage of monovalent and divalent cations such as magnesium, calcium, and zinc. TRPM7 is ubiquitously expressed and plays fundamental roles in cellular ion homeostasis, signal transduction, cell proliferation, migration, and stress response. Its kinase domain can phosphorylate multiple substrates, including nuclear histones. Physiologically, TRPM7 activity is tightly regulated by intracellular magnesium, ATP, and membrane PIP₂ levels. Dysregulation of TRPM7 is linked to cancer progression, ischemic injury, inflammation, and cardiovascular disease. Targeting TRPM7 presents therapeutic challenges due to its essential, broad biological roles and dual molecular functions.

Other names

TRPM7Transient receptor potential cation channel, subfamily M, member 7Channel-kinase TRPM7TRPM7 channel-kinase

Molecules can inhibit cation conductance through the channel pore (channel blockers). Inhibition of the intrinsic kinase domain (serine/threonine kinase activity). Modulation by physiological regulators: Mg²⁺, Mg·ATP, and phosphatidylinositol-4,5-bisphosphate (PIP₂) are endogenous inhibitors/regulators.