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Structural basis for promiscuous action of monoterpenes on TRP channels

Monoterpenes are major constituents of plant-derived essential oils and have long been widely used for therapeutic and cosmetic applications. The monoterpenes menthol and camphor are agonists or antagonists for several TRP channels such as TRPM8, TRPV1, TRPV3 and TRPA1. However, which regions within...

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Autores principales: Nguyen, Thi Hong Dung, Itoh, Satoru G., Okumura, Hisashi, Tominaga, Makoto
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7935860/
https://www.ncbi.nlm.nih.gov/pubmed/33674682
http://dx.doi.org/10.1038/s42003-021-01776-0
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author Nguyen, Thi Hong Dung
Itoh, Satoru G.
Okumura, Hisashi
Tominaga, Makoto
author_facet Nguyen, Thi Hong Dung
Itoh, Satoru G.
Okumura, Hisashi
Tominaga, Makoto
author_sort Nguyen, Thi Hong Dung
collection PubMed
description Monoterpenes are major constituents of plant-derived essential oils and have long been widely used for therapeutic and cosmetic applications. The monoterpenes menthol and camphor are agonists or antagonists for several TRP channels such as TRPM8, TRPV1, TRPV3 and TRPA1. However, which regions within TRPV1 and TRPV3 confer sensitivity to monoterpenes or other synthesized chemicals such as 2-APB are unclear. In this study we identified conserved arginine and glycine residues in the linker between S4 and S5 that are related to the action of these chemicals and validated these findings in molecular dynamics simulations. The involvement of these amino acids differed between TRPV3 and TRPV1 for chemical-induced and heat-evoked activation. These findings provide the basis for characterization of physiological function and biophysical properties of ion channels.
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spelling pubmed-79358602021-03-19 Structural basis for promiscuous action of monoterpenes on TRP channels Nguyen, Thi Hong Dung Itoh, Satoru G. Okumura, Hisashi Tominaga, Makoto Commun Biol Article Monoterpenes are major constituents of plant-derived essential oils and have long been widely used for therapeutic and cosmetic applications. The monoterpenes menthol and camphor are agonists or antagonists for several TRP channels such as TRPM8, TRPV1, TRPV3 and TRPA1. However, which regions within TRPV1 and TRPV3 confer sensitivity to monoterpenes or other synthesized chemicals such as 2-APB are unclear. In this study we identified conserved arginine and glycine residues in the linker between S4 and S5 that are related to the action of these chemicals and validated these findings in molecular dynamics simulations. The involvement of these amino acids differed between TRPV3 and TRPV1 for chemical-induced and heat-evoked activation. These findings provide the basis for characterization of physiological function and biophysical properties of ion channels. Nature Publishing Group UK 2021-03-05 /pmc/articles/PMC7935860/ /pubmed/33674682 http://dx.doi.org/10.1038/s42003-021-01776-0 Text en © The Author(s) 2021 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Article
Nguyen, Thi Hong Dung
Itoh, Satoru G.
Okumura, Hisashi
Tominaga, Makoto
Structural basis for promiscuous action of monoterpenes on TRP channels
title Structural basis for promiscuous action of monoterpenes on TRP channels
title_full Structural basis for promiscuous action of monoterpenes on TRP channels
title_fullStr Structural basis for promiscuous action of monoterpenes on TRP channels
title_full_unstemmed Structural basis for promiscuous action of monoterpenes on TRP channels
title_short Structural basis for promiscuous action of monoterpenes on TRP channels
title_sort structural basis for promiscuous action of monoterpenes on trp channels
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7935860/
https://www.ncbi.nlm.nih.gov/pubmed/33674682
http://dx.doi.org/10.1038/s42003-021-01776-0
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