Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels

Inhibitory potassium channels of the TREK1/TRAAK family are integrators of multiple stimuli, including temperature, membrane stretch, polyunsaturated fatty acids and pH. How these signals affect the gating of these channels is the subject of intense research. We have previously identified a cytoplas...

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Autores principales:	Frank S Choveau, Ismail Ben Soussia, Delphine Bichet, Chatelain C. Franck, Sylvain Feliciangeli, Florian Lesage
Formato:	article
Lenguaje:	EN
Publicado:	Frontiers Media S.A. 2021
Materias:	two-pore domain potassium channels pore gating openers allostery extracellular pH Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/07d33a38848c4d0183ced9c73c1ad2aa
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spelling	oai:doaj.org-article:07d33a38848c4d0183ced9c73c1ad2aa2021-11-16T14:20:34ZConvergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels1663-981210.3389/fphar.2021.755826https://doaj.org/article/07d33a38848c4d0183ced9c73c1ad2aa2021-09-01T00:00:00Zhttps://www.frontiersin.org/articles/10.3389/fphar.2021.755826/fullhttps://doaj.org/toc/1663-9812Inhibitory potassium channels of the TREK1/TRAAK family are integrators of multiple stimuli, including temperature, membrane stretch, polyunsaturated fatty acids and pH. How these signals affect the gating of these channels is the subject of intense research. We have previously identified a cytoplasmic domain, pCt, which plays a major role in controlling channel activity. Here, we use pharmacology to show that the effects of pCt, arachidonic acid, and extracellular pH converge to the same gate within the channel. Using a state-dependent inhibitor, fluoxetine, as well as natural and synthetic openers, we provide further evidence that the “up” and “down” conformations identified by crystallography do not correspond to open and closed states of these channels.Frank S ChoveauIsmail Ben SoussiaDelphine BichetChatelain C. FranckSylvain FeliciangeliFlorian LesageFrontiers Media S.A.articletwo-pore domain potassium channelspore gatingopenersallosteryextracellular pHTherapeutics. PharmacologyRM1-950ENFrontiers in Pharmacology, Vol 12 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	two-pore domain potassium channels pore gating openers allostery extracellular pH Therapeutics. Pharmacology RM1-950
spellingShingle	two-pore domain potassium channels pore gating openers allostery extracellular pH Therapeutics. Pharmacology RM1-950 Frank S Choveau Ismail Ben Soussia Delphine Bichet Chatelain C. Franck Sylvain Feliciangeli Florian Lesage Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels
description	Inhibitory potassium channels of the TREK1/TRAAK family are integrators of multiple stimuli, including temperature, membrane stretch, polyunsaturated fatty acids and pH. How these signals affect the gating of these channels is the subject of intense research. We have previously identified a cytoplasmic domain, pCt, which plays a major role in controlling channel activity. Here, we use pharmacology to show that the effects of pCt, arachidonic acid, and extracellular pH converge to the same gate within the channel. Using a state-dependent inhibitor, fluoxetine, as well as natural and synthetic openers, we provide further evidence that the “up” and “down” conformations identified by crystallography do not correspond to open and closed states of these channels.
format	article
author	Frank S Choveau Ismail Ben Soussia Delphine Bichet Chatelain C. Franck Sylvain Feliciangeli Florian Lesage
author_facet	Frank S Choveau Ismail Ben Soussia Delphine Bichet Chatelain C. Franck Sylvain Feliciangeli Florian Lesage
author_sort	Frank S Choveau
title	Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels
title_short	Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels
title_full	Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels
title_fullStr	Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels
title_full_unstemmed	Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels
title_sort	convergence of multiple stimuli to a single gate in trek1 and traak potassium channels
publisher	Frontiers Media S.A.
publishDate	2021
url	https://doaj.org/article/07d33a38848c4d0183ced9c73c1ad2aa
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Convergence of Multiple Stimuli to a Single Gate in TREK1 and TRAAK Potassium Channels

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