Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist

Calcium-activated chloride channels (CaCCs) play important roles in many physiological processes and their malfunction is implicated in diverse pathologies such as cancer, asthma, and hypertension. TMEM16A and TMEM16B proteins are the structural components of the CaCCs. Recent studies in cell cultur...

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Autores principales:	Adan Hernandez, Alfredo Alaniz-Palacios, Juan A. Contreras-Vite, Ataúlfo Martínez-Torres
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	Calcium-activated chloride channels TMEM16B channels TRPV4 antagonist Biology (General) QH301-705.5 Biochemistry QD415-436
Acceso en línea:	https://doaj.org/article/b7b76b4446b24c03b4ed390aaefd9509
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spelling	oai:doaj.org-article:b7b76b4446b24c03b4ed390aaefd95092021-12-04T04:35:22ZPositive modulation of the TMEM16B mediated currents by TRPV4 antagonist2405-580810.1016/j.bbrep.2021.101180https://doaj.org/article/b7b76b4446b24c03b4ed390aaefd95092021-12-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S2405580821002740https://doaj.org/toc/2405-5808Calcium-activated chloride channels (CaCCs) play important roles in many physiological processes and their malfunction is implicated in diverse pathologies such as cancer, asthma, and hypertension. TMEM16A and TMEM16B proteins are the structural components of the CaCCs. Recent studies in cell cultures and animal models have demonstrated that pharmacological inhibition of CaCCs could be helpful in the treatment of some diseases, however, there are few specific modulators of these channels. CaCCs and Transient Receptor Potential Vanilloid-4 (TRPV4) channels are co-expressed in some tissues where they functionally interact. TRPV4 is activated by different stimuli and forms a calcium permeable channel that is activated by GSK1016790A and antagonized by GSK2193874. Here we report that GSK2193874 enhances the chloride currents mediated by TMEM16B expressed in HEK cells at nanomolar concentrations and that GSK1016790A enhances native CaCCs of Xenopus oocytes. Thus, these compounds may be used as a tool for the study of CaCCs, TRPV4 and their interactions.Adan HernandezAlfredo Alaniz-PalaciosJuan A. Contreras-ViteAtaúlfo Martínez-TorresElsevierarticleCalcium-activated chloride channelsTMEM16B channelsTRPV4 antagonistBiology (General)QH301-705.5BiochemistryQD415-436ENBiochemistry and Biophysics Reports, Vol 28, Iss , Pp 101180- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Calcium-activated chloride channels TMEM16B channels TRPV4 antagonist Biology (General) QH301-705.5 Biochemistry QD415-436
spellingShingle	Calcium-activated chloride channels TMEM16B channels TRPV4 antagonist Biology (General) QH301-705.5 Biochemistry QD415-436 Adan Hernandez Alfredo Alaniz-Palacios Juan A. Contreras-Vite Ataúlfo Martínez-Torres Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist
description	Calcium-activated chloride channels (CaCCs) play important roles in many physiological processes and their malfunction is implicated in diverse pathologies such as cancer, asthma, and hypertension. TMEM16A and TMEM16B proteins are the structural components of the CaCCs. Recent studies in cell cultures and animal models have demonstrated that pharmacological inhibition of CaCCs could be helpful in the treatment of some diseases, however, there are few specific modulators of these channels. CaCCs and Transient Receptor Potential Vanilloid-4 (TRPV4) channels are co-expressed in some tissues where they functionally interact. TRPV4 is activated by different stimuli and forms a calcium permeable channel that is activated by GSK1016790A and antagonized by GSK2193874. Here we report that GSK2193874 enhances the chloride currents mediated by TMEM16B expressed in HEK cells at nanomolar concentrations and that GSK1016790A enhances native CaCCs of Xenopus oocytes. Thus, these compounds may be used as a tool for the study of CaCCs, TRPV4 and their interactions.
format	article
author	Adan Hernandez Alfredo Alaniz-Palacios Juan A. Contreras-Vite Ataúlfo Martínez-Torres
author_facet	Adan Hernandez Alfredo Alaniz-Palacios Juan A. Contreras-Vite Ataúlfo Martínez-Torres
author_sort	Adan Hernandez
title	Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist
title_short	Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist
title_full	Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist
title_fullStr	Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist
title_full_unstemmed	Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist
title_sort	positive modulation of the tmem16b mediated currents by trpv4 antagonist
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/b7b76b4446b24c03b4ed390aaefd9509
work_keys_str_mv	AT adanhernandez positivemodulationofthetmem16bmediatedcurrentsbytrpv4antagonist AT alfredoalanizpalacios positivemodulationofthetmem16bmediatedcurrentsbytrpv4antagonist AT juanacontrerasvite positivemodulationofthetmem16bmediatedcurrentsbytrpv4antagonist AT ataulfomartineztorres positivemodulationofthetmem16bmediatedcurrentsbytrpv4antagonist
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Positive modulation of the TMEM16B mediated currents by TRPV4 antagonist

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