Structural highlights
4xnx is a 3 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , , , |
| Related: | 4m48, 4xp1, 4xp4, 4xp5, 4xp6, 4xp9, 4xpa, 4xpb, 4xpf, 4xpg, 4xph, 4xpt |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
Most 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.
References
- ↑ Penmatsa A, Wang KH, Gouaux E. X-ray structures of Drosophila dopamine transporter in complex with nisoxetine and reboxetine. Nat Struct Mol Biol. 2015 May 11. doi: 10.1038/nsmb.3029. PMID:25961798 doi:http://dx.doi.org/10.1038/nsmb.3029
