The mechanism of a high-affinity allosteric inhibitor of the serotonin transporter

Per Plenge; Ara M. Abramyan; Gunnar Sørensen; Arne Mørk; Pia Weikop; Ulrik Gether; Benny Bang-Andersen; Lei Shi; Claus J. Loland

doi:10.1038/s41467-020-15292-y

Nature Communications (Mar 2020)

The mechanism of a high-affinity allosteric inhibitor of the serotonin transporter

Per Plenge,
Ara M. Abramyan,
Gunnar Sørensen,
Arne Mørk,
Pia Weikop,
Ulrik Gether,
Benny Bang-Andersen,
Lei Shi,
Claus J. Loland

Affiliations

Per Plenge: Laboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of Copenhagen
Ara M. Abramyan: Computational Chemistry and Molecular Biophysics Unit, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse—Intramural Research Program, National Institutes of Health
Gunnar Sørensen: Lundbeck Research, H. Lundbeck A/S
Arne Mørk: Lundbeck Research, H. Lundbeck A/S
Pia Weikop: Laboratory of Neuropsychiatry, Psychiatric Centre Copenhagen, University of Copenhagen
Ulrik Gether: Department of Neuroscience, Faculty of Health and Medical Sciences, University of Copenhagen
Benny Bang-Andersen: Lundbeck Research, H. Lundbeck A/S
Lei Shi: Computational Chemistry and Molecular Biophysics Unit, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse—Intramural Research Program, National Institutes of Health
Claus J. Loland: Laboratory for Membrane Protein Dynamics. Department of Neuroscience, Faculty of Health and Medical Sciences, University of Copenhagen

DOI: https://doi.org/10.1038/s41467-020-15292-y
Journal volume & issue: Vol. 11, no. 1
pp. 1 – 12

Abstract

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The serotonin transporter (SERT) terminates serotonin signaling and its activity is modulated by antidepressants. Here authors reveal the mechanistic details underlying the coupling between the two binding sites in SERT and a high-affinity ligand for the allosteric site.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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