DOI:10.1111/bph.13538 - Corpus ID: 25355417
Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122
@article{Leitner2016DirectMO,
title={Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122},
author={Michael G. Leitner and Niklas Michel and Marc Behrendt and Marlen Dierich and Sandeep Dembla and Bettina U. Wilke and Maik Konrad and Moritz Lindner and Johannes Oberwinkler and Dominik Oliver},
journal={British Journal of Pharmacology},
year={2016},
volume={173},
pages={2555 - 2569},
url={https://api.semanticscholar.org/CorpusID:25355417}
}- M. Leitner Niklas Michel D. Oliver
- Published in British Journal of... 1 August 2016
- Biology, Chemistry
It is found that the most frequently employed PLC inhibitor, U73122, activates endogenous ionic currents in widely used cell lines and this work sets out to identify these U 73122‐sensitive ion channels.
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54 Citations
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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.
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The phospholipase C inhibitor U73122 is a potent agonist of the polymodal transient receptor potential ankyrin type 1 (TRPA1) receptor channel
The results indicate that U73122 is a potent and selective TRPA1 agonist and may present a novel lead compound for the development ofTRPA1-targeting drugs.
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PLCβ thus regulates TRPM3 and TRPM8 channels by masking phosphatidylinositol 4,5-bisphosphate with its C-terminal domain, and in this way blocks the biological activation of TRP3 andTRPM8, which require interaction with this phospholipid.
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Dysregulation of PLC activity has been implicated in several pathophysiological conditions, including cancer, cardiovascular diseases, and neurological disorders, and identification of new drug targets that can selectively modulate PLCActivity is important.
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