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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...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Nature Publishing Group UK
2021
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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. |
format | Online Article Text |
id | pubmed-7935860 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Nature Publishing Group UK |
record_format | MEDLINE/PubMed |
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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