Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site

Wright et al. report the first structure of a human TRPC1/4/5 channel in complex with a xanthine-based TRPC5 inhibitor Pico145. They find that Pico145 binds to a conserved lipid binding site of TRPC5, where it displaces a phospholipid. This study provides insights into the mechanism-of-action of xan...

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Autores principales:	David J. Wright, Katie J. Simmons, Rachel M. Johnson, David J. Beech, Stephen P. Muench, Robin S. Bon
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2020
Materias:	Biology (General) QH301-705.5
Acceso en línea:	https://doaj.org/article/a4fe404129504c4c9fa1e7487c3b639e
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spelling	oai:doaj.org-article:a4fe404129504c4c9fa1e7487c3b639e2021-12-02T12:30:50ZHuman TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site10.1038/s42003-020-01437-82399-3642https://doaj.org/article/a4fe404129504c4c9fa1e7487c3b639e2020-11-01T00:00:00Zhttps://doi.org/10.1038/s42003-020-01437-8https://doaj.org/toc/2399-3642Wright et al. report the first structure of a human TRPC1/4/5 channel in complex with a xanthine-based TRPC5 inhibitor Pico145. They find that Pico145 binds to a conserved lipid binding site of TRPC5, where it displaces a phospholipid. This study provides insights into the mechanism-of-action of xanthine-based TRPC1/4/5 modulators.David J. WrightKatie J. SimmonsRachel M. JohnsonDavid J. BeechStephen P. MuenchRobin S. BonNature PortfolioarticleBiology (General)QH301-705.5ENCommunications Biology, Vol 3, Iss 1, Pp 1-11 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	Biology (General) QH301-705.5
spellingShingle	Biology (General) QH301-705.5 David J. Wright Katie J. Simmons Rachel M. Johnson David J. Beech Stephen P. Muench Robin S. Bon Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site
description	Wright et al. report the first structure of a human TRPC1/4/5 channel in complex with a xanthine-based TRPC5 inhibitor Pico145. They find that Pico145 binds to a conserved lipid binding site of TRPC5, where it displaces a phospholipid. This study provides insights into the mechanism-of-action of xanthine-based TRPC1/4/5 modulators.
format	article
author	David J. Wright Katie J. Simmons Rachel M. Johnson David J. Beech Stephen P. Muench Robin S. Bon
author_facet	David J. Wright Katie J. Simmons Rachel M. Johnson David J. Beech Stephen P. Muench Robin S. Bon
author_sort	David J. Wright
title	Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site
title_short	Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site
title_full	Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site
title_fullStr	Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site
title_full_unstemmed	Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site
title_sort	human trpc5 structures reveal interaction of a xanthine-based trpc1/4/5 inhibitor with a conserved lipid binding site
publisher	Nature Portfolio
publishDate	2020
url	https://doaj.org/article/a4fe404129504c4c9fa1e7487c3b639e
work_keys_str_mv	AT davidjwright humantrpc5structuresrevealinteractionofaxanthinebasedtrpc145inhibitorwithaconservedlipidbindingsite AT katiejsimmons humantrpc5structuresrevealinteractionofaxanthinebasedtrpc145inhibitorwithaconservedlipidbindingsite AT rachelmjohnson humantrpc5structuresrevealinteractionofaxanthinebasedtrpc145inhibitorwithaconservedlipidbindingsite AT davidjbeech humantrpc5structuresrevealinteractionofaxanthinebasedtrpc145inhibitorwithaconservedlipidbindingsite AT stephenpmuench humantrpc5structuresrevealinteractionofaxanthinebasedtrpc145inhibitorwithaconservedlipidbindingsite AT robinsbon humantrpc5structuresrevealinteractionofaxanthinebasedtrpc145inhibitorwithaconservedlipidbindingsite
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Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site

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