ReviewAssessment of TRPM7 functions by drug-like small molecules

•TRPM7 is a plasma membrane ion channel linked to a cytosolic protein kinase domain.•TRPM7 plays a critical role in Ca2+ signaling and Ca2+ dependent cellular processes.•Small organic compounds acting as inhibitors or activators of the TRPM7 channel have been identified.•TRPM7 has been defined as a promising drug target.

Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a plasma membrane ion channel linked to a cytosolic protein kinase domain. Genetic inactivation of this bi-functional protein revealed its crucial role in Ca2+ signalling, Mg2+ metabolism, immune responses, cell motility, proliferation and differentiation. Malfunctions of TRPM7 are associated with anoxic neuronal death, cardiac fibrosis, tumour progression and macrothrombocytopenia. Recently, several groups have identified small organic compounds acting as inhibitors or activators of the TRPM7 channel. In follow-up studies, the identified TRPM7 modulators were successfully used to uncover new cellular functions of TRPM7 in situ including a crucial role of TRPM7 in Ca2+ signaling and Ca2+ dependent cellular processes. Hence, TRPM7 has been defined as a promising drug target. Here, we summarize the progress in this quickly developing field.

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