The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter
oleh: Per Plenge, Dongxue Yang, Kristine Salomon, Louise Laursen, Iris E. Kalenderoglou, Amy H. Newman, Eric Gouaux, Jonathan A. Coleman, Claus J. Loland
| Format: | Article |
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| Diterbitkan: | Nature Portfolio 2021-08-01 |
Deskripsi
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.