Journal
PHARMACEUTICALS
Volume 15, Issue 1, Pages -Publisher
MDPI
DOI: 10.3390/ph15010081
Keywords
TRPM4; SUR1; CBA; flufenamic acid; 9-phenanthrol; siRNA; antibody; TRPM4 activator; TRPM4 inhibitor
Categories
Funding
- National Research Development and Innovation Office [NKFIH-K115397, NKFIH-K138090, NKFIH-FK128116]
- European Union [GINOP-2.3.2-15-2016-00040, EFOP-3.6.2-16-2017-00006]
- European Regional Development Fund
- New National Excellence Program of the Ministry for Innovation and Technology from the National Research Development and Innovation Fund [UNKP-21-3, UNKP-20-2]
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This review discusses the pharmacological modulation of TRPM4, as well as the methods and functions of studying TRPM4.
Transient receptor potential melastatin 4 is a unique member of the TRPM protein family and, similarly to TRPM5, is Ca2+-sensitive and permeable to monovalent but not divalent cations. It is widely expressed in many organs and is involved in several functions by regulating the membrane potential and Ca2+ homeostasis in both excitable and non-excitable cells. This part of the review discusses the pharmacological modulation of TRPM4 by listing, comparing, and describing both endogenous and exogenous activators and inhibitors of the ion channel. Moreover, other strategies used to study TRPM4 functions are listed and described. These strategies include siRNA-mediated silencing of TRPM4, dominant-negative TRPM4 variants, and anti-TRPM4 antibodies. TRPM4 is receiving more and more attention and is likely to be the topic of research in the future.
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