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Cited by 425

The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.

Neurotransmitter and psychostimulant recognition by the dopamine transporter

Open access
Wang, Kevin H., Penmatsa, Aravind, Gouaux, Eric·2015·Nature

Abstract

Na+/Cl–-coupled biogenic amine transporters are the primary targets of therapeutic and abused drugs, ranging from antidepressants to the psychostimulants cocaine and amphetamines, and to their cognate substrates. Here we determine X-ray crystal structures of the Drosophila melanogaster dopamine transporter (dDAT) bound to its substrate dopamine, a substrate analogue 3,4-dichlorophenethylamine, the psychostimulants d-amphetamine and methamphetamine, or to cocaine and cocaine analogues. All ligands bind to the central binding site, located approximately halfway across the membrane bilayer, in close proximity to bound sodium and chloride ions. The central binding site recognizes three chemically distinct classes of ligands via conformational changes that accommodate varying sizes and shapes, thus illustrating molecular principles that distinguish substrates from inhibitors in biogenic amine transporters.

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Crossref · 10.1038/nature14431

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Metadata

Authors
Wang, K. H., Penmatsa, A., & Gouaux, E.
Venue
Nature
Published
2015-05
Volume
521
Issue
7552
Pages
322-327
ISSN
  • 0028-0836 (ISSN-L)
  • 1476-4687
OpenAlex
W2129495111
Cited by
425
References
5
FWCI
17.75
Type
journal article
Language
en
Open access
green

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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