Science and Research

Assessment of TRPM7 functions by drug-like small molecules

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 Ca(2+) signalling, Mg(2+) 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 Ca(2+) signaling and Ca(2+) dependent cellular processes. Hence, TRPM7 has been defined as a promising drug target. Here, we summarize the progress in this quickly developing field.

  • Chubanov, V.
  • Ferioli, S.
  • Gudermann, T.

Keywords

  • Animals
  • Calcium/*metabolism
  • Calcium Signaling
  • Cell Death/drug effects
  • Endomyocardial Fibrosis/drug therapy/*genetics/metabolism/pathology
  • Gene Expression Regulation
  • Genetic Diseases, X-Linked/drug therapy/genetics/metabolism/pathology
  • Humans
  • Hypoxia, Brain/drug therapy/*genetics/metabolism/pathology
  • Magnesium/metabolism
  • Mice
  • Neoplasms/drug therapy/genetics/metabolism/pathology
  • Neurons/cytology/metabolism/pathology
  • Small Molecule Libraries/*pharmacology
  • Structure-Activity Relationship
  • TRPM Cation Channels/agonists/antagonists & inhibitors/*genetics/metabolism
  • Thrombocytopenia/drug therapy/genetics/metabolism/pathology
  • *Calcium
  • *Magnesium
  • *TRP channel
  • *trpm6
  • *trpm7
  • *alpha-kinase
Publication details
DOI: 10.1016/j.ceca.2017.03.004
Journal: Cell Calcium
Pages: 166-173 
Work Type: Review
Location: CPC-M
Disease Area: General Lung and Other
Partner / Member: LMU
Access-Number: 28356194
See publication on PubMed

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