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

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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Main Authors: Per Plenge, Dongxue Yang, Kristine Salomon, Louise Laursen, Iris E. Kalenderoglou, Amy H. Newman, Eric Gouaux, Jonathan A. Coleman, Claus J. Loland
Format: Article
Language:English
Published: Nature Publishing Group 2021-08-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-021-25363-3
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spelling doaj-7e4dd1b8938f4697aed6a531fb670e572021-08-22T11:38:57ZengNature Publishing GroupNature Communications2041-17232021-08-0112111210.1038/s41467-021-25363-3The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporterPer Plenge0Dongxue Yang1Kristine Salomon2Louise Laursen3Iris E. Kalenderoglou4Amy H. Newman5Eric Gouaux6Jonathan A. Coleman7Claus J. Loland8Laboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of CopenhagenVollum Institute, Oregon Health & Science UniversityLaboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of CopenhagenLaboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of CopenhagenLaboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of CopenhagenMedicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse - Intramural Research Program, National Institutes of HealthVollum Institute, Oregon Health & Science UniversityVollum Institute, Oregon Health & Science UniversityLaboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of CopenhagenVilazodone (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.https://doi.org/10.1038/s41467-021-25363-3
collection DOAJ
language English
format Article
sources DOAJ
author Per Plenge
Dongxue Yang
Kristine Salomon
Louise Laursen
Iris E. Kalenderoglou
Amy H. Newman
Eric Gouaux
Jonathan A. Coleman
Claus J. Loland
spellingShingle 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
Nature Communications
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 Publishing Group
series Nature Communications
issn 2041-1723
publishDate 2021-08-01
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.
url https://doi.org/10.1038/s41467-021-25363-3
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