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) |
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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