Molecular pharmacology of the onco-TRP channel TRPV6

TRPV6, a representative of the vanilloid subfamily of TRP channels, serves as the principal calcium uptake channel in the gut. Dysregulation of TRPV6 results in disturbed calcium homeostasis leading to a variety of human diseases, including many forms of cancer. Inhibitors of this oncochannel are th...

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Detalles Bibliográficos
Autores principales: Neuberger, Arthur, Sobolevsky, Alexander I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2023
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10578198/
https://www.ncbi.nlm.nih.gov/pubmed/37838981
http://dx.doi.org/10.1080/19336950.2023.2266669
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author Neuberger, Arthur
Sobolevsky, Alexander I.
author_facet Neuberger, Arthur
Sobolevsky, Alexander I.
author_sort Neuberger, Arthur
collection PubMed
description TRPV6, a representative of the vanilloid subfamily of TRP channels, serves as the principal calcium uptake channel in the gut. Dysregulation of TRPV6 results in disturbed calcium homeostasis leading to a variety of human diseases, including many forms of cancer. Inhibitors of this oncochannel are therefore particularly needed. In this review, we provide an overview of recent advances in structural pharmacology that uncovered the molecular mechanisms of TRPV6 inhibition by a variety of small molecules, including synthetic and natural, plant-derived compounds as well as some prospective and clinically approved drugs.
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spelling pubmed-105781982023-10-17 Molecular pharmacology of the onco-TRP channel TRPV6 Neuberger, Arthur Sobolevsky, Alexander I. Channels (Austin) Review TRPV6, a representative of the vanilloid subfamily of TRP channels, serves as the principal calcium uptake channel in the gut. Dysregulation of TRPV6 results in disturbed calcium homeostasis leading to a variety of human diseases, including many forms of cancer. Inhibitors of this oncochannel are therefore particularly needed. In this review, we provide an overview of recent advances in structural pharmacology that uncovered the molecular mechanisms of TRPV6 inhibition by a variety of small molecules, including synthetic and natural, plant-derived compounds as well as some prospective and clinically approved drugs. Taylor & Francis 2023-10-15 /pmc/articles/PMC10578198/ /pubmed/37838981 http://dx.doi.org/10.1080/19336950.2023.2266669 Text en © 2023 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The terms on which this article has been published allow the posting of the Accepted Manuscript in a repository by the author(s) or with their consent.
spellingShingle Review
Neuberger, Arthur
Sobolevsky, Alexander I.
Molecular pharmacology of the onco-TRP channel TRPV6
title Molecular pharmacology of the onco-TRP channel TRPV6
title_full Molecular pharmacology of the onco-TRP channel TRPV6
title_fullStr Molecular pharmacology of the onco-TRP channel TRPV6
title_full_unstemmed Molecular pharmacology of the onco-TRP channel TRPV6
title_short Molecular pharmacology of the onco-TRP channel TRPV6
title_sort molecular pharmacology of the onco-trp channel trpv6
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10578198/
https://www.ncbi.nlm.nih.gov/pubmed/37838981
http://dx.doi.org/10.1080/19336950.2023.2266669
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