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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Bibliographic Details
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
Description
Summary: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.
ISSN:2041-1723

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