The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter

Vilazodone (VLZ) is a drug for the treatment of major depressive disorders that targets the serotonin transporter (SERT). Here, the authors combine pharmacology measurements and cryo-EM structural analysis to characterize VLZ binding to SERT and observe that VLZ exhibits non-competitive inhibition o...

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Autores principales:	Per Plenge, Dongxue Yang, Kristine Salomon, Louise Laursen, Iris E. Kalenderoglou, Amy H. Newman, Eric Gouaux, Jonathan A. Coleman, Claus J. Loland
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/7e4dd1b8938f4697aed6a531fb670e57
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spelling	oai:doaj.org-article:7e4dd1b8938f4697aed6a531fb670e572021-12-02T16:45:55ZThe antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter10.1038/s41467-021-25363-32041-1723https://doaj.org/article/7e4dd1b8938f4697aed6a531fb670e572021-08-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-25363-3https://doaj.org/toc/2041-1723Vilazodone (VLZ) is a drug for the treatment of major depressive disorders that targets the serotonin transporter (SERT). Here, the authors combine pharmacology measurements and cryo-EM structural analysis to characterize VLZ binding to SERT and observe that VLZ exhibits non-competitive inhibition of serotonin transport and binds with nanomolar affinity to an allosteric site in SERT.Per PlengeDongxue YangKristine SalomonLouise LaursenIris E. KalenderoglouAmy H. NewmanEric GouauxJonathan A. ColemanClaus J. LolandNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-12 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Per Plenge Dongxue Yang Kristine Salomon Louise Laursen Iris E. Kalenderoglou Amy H. Newman Eric Gouaux Jonathan A. Coleman Claus J. Loland The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
description	Vilazodone (VLZ) is a drug for the treatment of major depressive disorders that targets the serotonin transporter (SERT). Here, the authors combine pharmacology measurements and cryo-EM structural analysis to characterize VLZ binding to SERT and observe that VLZ exhibits non-competitive inhibition of serotonin transport and binds with nanomolar affinity to an allosteric site in SERT.
format	article
author	Per Plenge Dongxue Yang Kristine Salomon Louise Laursen Iris E. Kalenderoglou Amy H. Newman Eric Gouaux Jonathan A. Coleman Claus J. Loland
author_facet	Per Plenge Dongxue Yang Kristine Salomon Louise Laursen Iris E. Kalenderoglou Amy H. Newman Eric Gouaux Jonathan A. Coleman Claus J. Loland
author_sort	Per Plenge
title	The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
title_short	The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
title_full	The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
title_fullStr	The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
title_full_unstemmed	The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
title_sort	antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/7e4dd1b8938f4697aed6a531fb670e57
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The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter

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