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TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation

The transient receptor potential melastatin subtype 8 (TRPM8) is a cold sensor in humans, activated by low temperatures (>10, <28 °C), but also a polymodal ion channel, stimulated by voltage, pressure, cooling compounds (menthol, icilin), and hyperosmolarity. An increased number of experimenta...

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Autores principales: Izquierdo, Carolina, Martín-Martínez, Mercedes, Gómez-Monterrey, Isabel, González-Muñiz, Rosario
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8395166/
https://www.ncbi.nlm.nih.gov/pubmed/34445208
http://dx.doi.org/10.3390/ijms22168502
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author Izquierdo, Carolina
Martín-Martínez, Mercedes
Gómez-Monterrey, Isabel
González-Muñiz, Rosario
author_facet Izquierdo, Carolina
Martín-Martínez, Mercedes
Gómez-Monterrey, Isabel
González-Muñiz, Rosario
author_sort Izquierdo, Carolina
collection PubMed
description The transient receptor potential melastatin subtype 8 (TRPM8) is a cold sensor in humans, activated by low temperatures (>10, <28 °C), but also a polymodal ion channel, stimulated by voltage, pressure, cooling compounds (menthol, icilin), and hyperosmolarity. An increased number of experimental results indicate the implication of TRPM8 channels in cold thermal transduction and pain detection, transmission, and maintenance in different tissues and organs. These channels also have a repercussion on different kinds of life-threatening tumors and other pathologies, which include urinary and respiratory tract dysfunctions, dry eye disease, and obesity. This compendium firstly covers newly described papers on the expression of TRPM8 channels and their correlation with pathological states. An overview on the structural knowledge, after cryo-electron microscopy success in solving different TRPM8 structures, as well as some insights obtained from mutagenesis studies, will follow. Most recently described families of TRPM8 modulators are also covered, along with a section of molecules that have reached clinical trials. To finalize, authors provide an outline of the potential prospects in the TRPM8 field.
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spelling pubmed-83951662021-08-28 TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation Izquierdo, Carolina Martín-Martínez, Mercedes Gómez-Monterrey, Isabel González-Muñiz, Rosario Int J Mol Sci Review The transient receptor potential melastatin subtype 8 (TRPM8) is a cold sensor in humans, activated by low temperatures (>10, <28 °C), but also a polymodal ion channel, stimulated by voltage, pressure, cooling compounds (menthol, icilin), and hyperosmolarity. An increased number of experimental results indicate the implication of TRPM8 channels in cold thermal transduction and pain detection, transmission, and maintenance in different tissues and organs. These channels also have a repercussion on different kinds of life-threatening tumors and other pathologies, which include urinary and respiratory tract dysfunctions, dry eye disease, and obesity. This compendium firstly covers newly described papers on the expression of TRPM8 channels and their correlation with pathological states. An overview on the structural knowledge, after cryo-electron microscopy success in solving different TRPM8 structures, as well as some insights obtained from mutagenesis studies, will follow. Most recently described families of TRPM8 modulators are also covered, along with a section of molecules that have reached clinical trials. To finalize, authors provide an outline of the potential prospects in the TRPM8 field. MDPI 2021-08-07 /pmc/articles/PMC8395166/ /pubmed/34445208 http://dx.doi.org/10.3390/ijms22168502 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Izquierdo, Carolina
Martín-Martínez, Mercedes
Gómez-Monterrey, Isabel
González-Muñiz, Rosario
TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
title TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
title_full TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
title_fullStr TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
title_full_unstemmed TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
title_short TRPM8 Channels: Advances in Structural Studies and Pharmacological Modulation
title_sort trpm8 channels: advances in structural studies and pharmacological modulation
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8395166/
https://www.ncbi.nlm.nih.gov/pubmed/34445208
http://dx.doi.org/10.3390/ijms22168502
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