Abstract
Most antidepressants elicit their therapeutic benefits through selective blockade of Na + /Cl â -coupled neurotransmitter transporters. Here we report X-ray structures of the Drosophila melanogaster dopamine transporter in complexes with the polycyclic antidepressants nisoxetine or reboxetine. The inhibitors stabilize the transporter in an outward-open conformation by occupying the substrate-binding site. These structures explain how interactions between the binding pocket and substituents on the aromatic rings of antidepressants modulate drug-transporter selectivity.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 506-508 |
| Number of pages | 3 |
| Journal | Nature Structural and Molecular Biology |
| Volume | 22 |
| Issue number | 6 |
| DOIs | |
| State | Published - Jun 3 2015 |
ASJC Scopus subject areas
- Structural Biology
- Molecular Biology
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Penmatsa, A., Wang, K. H., & Gouaux, E. (2015). X-ray structures of Drosophila dopamine transporter in complex with nisoxetine and reboxetine. Nature Structural and Molecular Biology, 22(6), 506-508. https://doi.org/10.1038/nsmb.3029