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4XP1

X-ray structure of Drosophila dopamine transporter bound to neurotransmitter dopamine

Summary for 4XP1
Entry DOI10.2210/pdb4xp1/pdb
Related4XNX 4XP4 4XP5 4XP6 4XP9 4XPA 4XPB 4XPF 4XPG 4XPH 4XPT
Related PRD IDPRD_900001
DescriptorDopamine transporter, isoform B, 1,2-ETHANEDIOL, CHOLESTEROL HEMISUCCINATE, ... (13 entities in total)
Functional Keywordsintegral membrane protein, membrane protein-transport protein complex, membrane protein/transport protein
Biological sourceDrosophila melanogaster (Fruit fly)
More
Total number of polymer chains3
Total formula weight109207.51
Authors
Gouaux, E.,Penmatsa, A.,Wang, K. (deposition date: 2015-01-16, release date: 2015-05-06, Last modification date: 2024-10-09)
Primary citationWang, K.H.,Penmatsa, A.,Gouaux, E.
Neurotransmitter and psychostimulant recognition by the dopamine transporter.
Nature, 521:322-327, 2015
Cited by
PubMed 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.
PubMed: 25970245
DOI: 10.1038/nature14431
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.89 Å)
Structure validation

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