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X-ray structure of Drosophila dopamine transporter in complex with nisoxetineX-ray structure of Drosophila dopamine transporter in complex with nisoxetine
Structural highlights
Publication Abstract from PubMedMost antidepressants elicit their therapeutic benefits through selective blockade of Na+/Cl--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. X-ray structures of Drosophila dopamine transporter in complex with nisoxetine and reboxetine.,Penmatsa A, Wang KH, Gouaux E Nat Struct Mol Biol. 2015 May 11. doi: 10.1038/nsmb.3029. PMID:25961798[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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