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

Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a unique bifunctional protein, often referred to as a chanzyme, because it contains both a non-selective cation channel and a C-terminal alpha-type serine/threonine protein kinase domain (UniProt Q96QT4). It is ubiquitously expressed and serves as a primary regulator of magnesium (Mg2+) and calcium (Ca2+) homeostasis, which are essential for cellular metabolism, proliferation, and survival (PubMed: 11385574). TRPM7 is significantly involved in various diseases; for instance, its overexpression is linked to increased cell proliferation and metastasis in several cancers, including breast and pancreatic cancer (PubMed: 23533610). In the cardiovascular system, TRPM7 contributes to vascular remodeling, hypertension, and atrial fibrillation (PubMed: 21835247). Additionally, TRPM7 has been implicated in neurodegenerative processes and ischemic brain injury, where its activation contributes to neuronal cell death (PubMed: 17347445). Pharmacological targeting of TRPM7 typically involves small-molecule inhibitors like NS8593 or natural products like Waixenicin A, which aim to block the channel's pore or inhibit its kinase activity to treat fibroproliferative and malignant conditions (PubMed: 20610744, PubMed: 21430222).

Other names

TRP-PLIKChaK1LTRPC7ALSPG17Transient receptor potential-protein kinaseChannel-kinase 1

Inhibition of the cation channel pore to prevent magnesium and calcium influx, or inhibition of the C-terminal alpha-kinase domain to disrupt downstream signaling pathways.