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Assessment of TRPM7 functions by drug-like small molecules.
- Source :
-
Cell calcium [Cell Calcium] 2017 Nov; Vol. 67, pp. 166-173. Date of Electronic Publication: 2017 Mar 14. - Publication Year :
- 2017
-
Abstract
- 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 <superscript>2+</superscript> signalling, Mg <superscript>2+</superscript> 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 <superscript>2+</superscript> signaling and Ca <superscript>2+</superscript> dependent cellular processes. Hence, TRPM7 has been defined as a promising drug target. Here, we summarize the progress in this quickly developing field.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Calcium Signaling
Cell Death drug effects
Endomyocardial Fibrosis drug therapy
Endomyocardial Fibrosis metabolism
Endomyocardial Fibrosis pathology
Gene Expression Regulation
Genetic Diseases, X-Linked drug therapy
Genetic Diseases, X-Linked genetics
Genetic Diseases, X-Linked metabolism
Genetic Diseases, X-Linked pathology
Humans
Hypoxia, Brain drug therapy
Hypoxia, Brain metabolism
Hypoxia, Brain pathology
Magnesium metabolism
Mice
Neoplasms drug therapy
Neoplasms genetics
Neoplasms metabolism
Neoplasms pathology
Neurons cytology
Neurons metabolism
Neurons pathology
Structure-Activity Relationship
TRPM Cation Channels agonists
TRPM Cation Channels antagonists & inhibitors
TRPM Cation Channels metabolism
Thrombocytopenia drug therapy
Thrombocytopenia genetics
Thrombocytopenia metabolism
Thrombocytopenia pathology
Calcium metabolism
Endomyocardial Fibrosis genetics
Hypoxia, Brain genetics
Small Molecule Libraries pharmacology
TRPM Cation Channels genetics
Subjects
Details
- Language :
- English
- ISSN :
- 1532-1991
- Volume :
- 67
- Database :
- MEDLINE
- Journal :
- Cell calcium
- Publication Type :
- Academic Journal
- Accession number :
- 28356194
- Full Text :
- https://doi.org/10.1016/j.ceca.2017.03.004