Cargando…

Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease

Proteins of the TRPC family can form many homo- and heterotetrameric cation channels permeable to Na(+), K(+) and Ca(2+). In this review, we focus on channels formed by the isoforms TRPC1, TRPC4 and TRPC5. We review evidence for the formation of different TRPC1/4/5 tetramers, give an overview of rec...

Descripción completa

Detalles Bibliográficos
Autores principales: Minard, Aisling, Bauer, Claudia C., Wright, David J., Rubaiy, Hussein N., Muraki, Katsuhiko, Beech, David J., Bon, Robin S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6025525/
https://www.ncbi.nlm.nih.gov/pubmed/29865154
http://dx.doi.org/10.3390/cells7060052
_version_ 1783336299997954048
author Minard, Aisling
Bauer, Claudia C.
Wright, David J.
Rubaiy, Hussein N.
Muraki, Katsuhiko
Beech, David J.
Bon, Robin S.
author_facet Minard, Aisling
Bauer, Claudia C.
Wright, David J.
Rubaiy, Hussein N.
Muraki, Katsuhiko
Beech, David J.
Bon, Robin S.
author_sort Minard, Aisling
collection PubMed
description Proteins of the TRPC family can form many homo- and heterotetrameric cation channels permeable to Na(+), K(+) and Ca(2+). In this review, we focus on channels formed by the isoforms TRPC1, TRPC4 and TRPC5. We review evidence for the formation of different TRPC1/4/5 tetramers, give an overview of recently developed small-molecule TRPC1/4/5 activators and inhibitors, highlight examples of biological roles of TRPC1/4/5 channels in different tissues and pathologies, and discuss how high-quality chemical probes of TRPC1/4/5 modulators can be used to understand the involvement of TRPC1/4/5 channels in physiological and pathophysiological processes.
format Online
Article
Text
id pubmed-6025525
institution National Center for Biotechnology Information
language English
publishDate 2018
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-60255252018-07-09 Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease Minard, Aisling Bauer, Claudia C. Wright, David J. Rubaiy, Hussein N. Muraki, Katsuhiko Beech, David J. Bon, Robin S. Cells Review Proteins of the TRPC family can form many homo- and heterotetrameric cation channels permeable to Na(+), K(+) and Ca(2+). In this review, we focus on channels formed by the isoforms TRPC1, TRPC4 and TRPC5. We review evidence for the formation of different TRPC1/4/5 tetramers, give an overview of recently developed small-molecule TRPC1/4/5 activators and inhibitors, highlight examples of biological roles of TRPC1/4/5 channels in different tissues and pathologies, and discuss how high-quality chemical probes of TRPC1/4/5 modulators can be used to understand the involvement of TRPC1/4/5 channels in physiological and pathophysiological processes. MDPI 2018-06-01 /pmc/articles/PMC6025525/ /pubmed/29865154 http://dx.doi.org/10.3390/cells7060052 Text en © 2018 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Minard, Aisling
Bauer, Claudia C.
Wright, David J.
Rubaiy, Hussein N.
Muraki, Katsuhiko
Beech, David J.
Bon, Robin S.
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
title Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
title_full Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
title_fullStr Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
title_full_unstemmed Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
title_short Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
title_sort remarkable progress with small-molecule modulation of trpc1/4/5 channels: implications for understanding the channels in health and disease
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6025525/
https://www.ncbi.nlm.nih.gov/pubmed/29865154
http://dx.doi.org/10.3390/cells7060052
work_keys_str_mv AT minardaisling remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease
AT bauerclaudiac remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease
AT wrightdavidj remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease
AT rubaiyhusseinn remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease
AT murakikatsuhiko remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease
AT beechdavidj remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease
AT bonrobins remarkableprogresswithsmallmoleculemodulationoftrpc145channelsimplicationsforunderstandingthechannelsinhealthanddisease