The binding sites for cocaine and dopamine in the dopamine transporter overlap.
paper
Cited
Public
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- Authors
- Beuming, Thijs; Kniazeff, Julie; Bergmann, Marianne L; Shi, Lei; Gracia, Luis; Raniszewska, Klaudia; Newman, Amy Hauck; Javitch, Jonathan A; Weinstein, Harel; Gether, Ulrik; Loland, Claus J
- Year
- 2008
- Journal
- Nature neuroscience
- PMID
- 18568020
- DOI
- 10.1038/nn.2146
- PMCID
- PMC2692229
Cocaine is a widely abused substance with psychostimulant effects that are attributed to inhibition of the dopamine transporter (DAT). We present molecular models for DAT binding of cocaine and cocaine analogs constructed from the high-resolution structure of the bacterial transporter homolog LeuT. Our models suggest that the binding site for cocaine and cocaine analogs is deeply buried between transmembrane segments 1, 3, 6 and 8, and overlaps with the binding sites for the substrates dopamine and amphetamine, as well as for benztropine-like DAT inhibitors. We validated our models by detailed mutagenesis and by trapping the radiolabeled cocaine analog [3H]CFT in the transporter, either by cross-linking engineered cysteines or with an engineered Zn2+-binding site that was situated extracellularly to the predicted common binding pocket. Our data demonstrate the molecular basis for the competitive inhibition of dopamine transport by cocaine.
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| Title | Year | PMID |
|---|---|---|
| The aggregate effect of dopamine genes on dependence symptoms among cocaine users: cross-validation of a candidate system scoring approach. | 2012 | 22358648 |
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| Non-dioxin-like PCBs inhibit [(3)H]WIN-35,428 binding to the dopamine transporter: a structure-activity relationship study. | Wigestrand MB et al. | β | 2013 | β |
| Phosphorylation of dopamine transporter serine 7 modulates cocaine analog binding. | Moritz AE et al. | β | 2013 | β |
| The cost of living in the membrane: a case study of hydrophobic mismatch for the multi-segment protein LeuT. | Mondal S et al. | β | 2013 | β |
| The role of cysteines and histidins of the norepinephrine transporter. | Wenge B et al. | β | 2013 | β |
| X-ray structure of dopamine transporter elucidates antidepressant mechanism. | Penmatsa A et al. | β | 2013 | β |
| 4-Methylthioamphetamine increases dopamine in the rat striatum and has rewarding effects in vivo. | Sotomayor-ZΓ‘rate R et al. | β | 2012 | β |
| Amino acid secondary transporters: toward a common transport mechanism. | Schweikhard ES et al. | β | 2012 | β |
| A second extracellular site is required for norepinephrine transport by the human norepinephrine transporter. | Wang CI et al. | β | 2012 | β |
| Atomistic models of ion and solute transport by the sodium-dependent secondary active transporters. | Zdravkovic I et al. | β | 2012 | β |
| Binding of the amphetamine-like 1-phenyl-piperazine to monoamine transporters. | Severinsen K et al. | β | 2012 | β |
| Characterization of [Β³H]CFT binding to the norepinephrine transporter suggests that binding of CFT and nisoxetine is not mutually exclusive. | Zhen J et al. | β | 2012 | β |
| Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (Β±)-threo-Methylphenidate. | Lapinsky DJ et al. | β | 2012 | β |
| High selectivity of the Ξ³-aminobutyric acid transporter 2 (GAT-2, SLC6A13) revealed by structure-based approach. | Schlessinger A et al. | β | 2012 | β |
| Insights from molecular dynamics: the binding site of cocaine in the dopamine transporter and permeation pathways of substrates in the leucine and dopamine transporters. | Merchant BA et al. | β | 2012 | β |
| Interaction of antidepressants with the serotonin and norepinephrine transporters: mutational studies of the S1 substrate binding pocket. | SΓΈrensen L et al. | β | 2012 | β |
| Ligand-dependent conformations and dynamics of the serotonin 5-HT(2A) receptor determine its activation and membrane-driven oligomerization properties. | Shan J et al. | β | 2012 | β |
| Modeling of pharmacokinetics of cocaine in human reveals the feasibility for development of enzyme therapies for drugs of abuse. | Zheng F et al. | β | 2012 | β |
| Monoamine transporter structure, function, dynamics, and drug discovery: a computational perspective. | Manepalli S et al. | β | 2012 | β |
| Novel C-1 substituted cocaine analogs unlike cocaine or benztropine. | Reith ME et al. | β | 2012 | β |
| R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse. | Loland CJ et al. | β | 2012 | β |
| Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter. | Plenge P et al. | β | 2012 | β |
| Structures of LeuT in bicelles define conformation and substrate binding in a membrane-like context. | Wang H et al. | β | 2012 | β |
| The aggregate effect of dopamine genes on dependence symptoms among cocaine users: cross-validation of a candidate system scoring approach. | Derringer J et al. | β | 2012 | β |
| The mechanistic basis for noncompetitive ibogaine inhibition of serotonin and dopamine transporters. | Bulling S et al. | β | 2012 | β |
| The solute carrier 6 family of transporters. | BrΓΆer S et al. | β | 2012 | β |
| A catecholamine transporter from the human parasite Schistosoma mansoni with low affinity for psychostimulants. | Larsen MB et al. | β | 2011 | β |
| A conserved asparagine residue in transmembrane segment 1 (TM1) of serotonin transporter dictates chloride-coupled neurotransmitter transport. | Henry LK et al. | β | 2011 | β |
| Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling. | Lapinsky DJ et al. | β | 2011 | β |
| Cocaine-insensitive dopamine transporters with intact substrate transport produced by self-administration. | Ferris MJ et al. | β | 2011 | β |
| Computational methods for the discovery of mood disorder therapies. | LΓ³pez-Vallejo F et al. | β | 2011 | β |
| Cytoplasmic permeation pathway of neurotransmitter transporters. | Rudnick G | β | 2011 | β |
| Dopamine release mediated by the dopamine transporter, facts and consequences. | Leviel V | β | 2011 | β |
| Enzyme-therapy approaches for the treatment of drug overdose and addiction. | Zheng F et al. | β | 2011 | β |
| Identification of a novel selective serotonin reuptake inhibitor by coupling monoamine transporter-based virtual screening and rational molecular hybridization. | Nolan TL et al. | β | 2011 | β |
| Interaction of tyrosine 151 in norepinephrine transporter with the 2Ξ² group of cocaine analog RTI-113. | Hill ER et al. | β | 2011 | β |
| Modeling and simulation of ion-coupled and ATP-driven membrane proteins. | Faraldo-GΓ³mez JD et al. | β | 2011 | β |
| N-substituted benztropine analogs: selective dopamine transporter ligands with a fast onset of action and minimal cocaine-like behavioral effects. | Li SM et al. | β | 2011 | β |
| Site-directed mutations near transmembrane domain 1 alter conformation and function of norepinephrine and dopamine transporters. | Guptaroy B et al. | β | 2011 | β |
| SKF-83566, a D1-dopamine receptor antagonist, inhibits the dopamine transporter. | Stouffer MA et al. | β | 2011 | β |
| SLC6 neurotransmitter transporters: structure, function, and regulation. | Kristensen AS et al. | β | 2011 | β |
| Structure-based discovery of prescription drugs that interact with the norepinephrine transporter, NET. | Schlessinger A et al. | β | 2011 | β |
| Substrate recognition and translocation by polyspecific organic cation transporters. | Koepsell H | β | 2011 | β |
| The atypical stimulant and nootropic modafinil interacts with the dopamine transporter in a different manner than classical cocaine-like inhibitors. | Schmitt KC et al. | β | 2011 | β |
| The binding sites for benztropines and dopamine in the dopamine transporter overlap. | Bisgaard H et al. | β | 2011 | β |
| Therapeutic-like properties of a dopamine uptake inhibitor in animal models of amphetamine addiction. | Velazquez-Sanchez C et al. | β | 2011 | β |
| The substrate-driven transition to an inward-facing conformation in the functional mechanism of the dopamine transporter. | Shan J et al. | β | 2011 | β |
| Unbiased simulations reveal the inward-facing conformation of the human serotonin transporter and Na(+) ion release. | KoldsΓΈ H et al. | β | 2011 | β |
| A tryptamine-derived catecholaminergic enhancer, (-)-1-(benzofuran-2-yl)-2-propylaminopentane [(-)-BPAP], attenuates reinstatement of methamphetamine-seeking behavior in rats. | Hiranita T et al. | β | 2010 | β |
| Binding and orientation of tricyclic antidepressants within the central substrate site of the human serotonin transporter. | Sinning S et al. | β | 2010 | β |
| Bivalent phenethylamines as novel dopamine transporter inhibitors: evidence for multiple substrate-binding sites in a single transporter. | Schmitt KC et al. | β | 2010 | β |
| Comparison of human solute carriers. | Schlessinger A et al. | β | 2010 | β |
| Direct involvement of sigma-1 receptors in the dopamine D1 receptor-mediated effects of cocaine. | Navarro G et al. | β | 2010 | β |
| Dopamine transporter-dependent and -independent striatal binding of the benztropine analog JHW 007, a cocaine antagonist with low abuse liability. | Kopajtic TA et al. | β | 2010 | β |
| Dopamine uptake inhibitors but not dopamine releasers induce greater increases in motor behavior and extracellular dopamine in adolescent rats than in adult male rats. | Walker QD et al. | β | 2010 | β |
| Emerging structure-function relationships defining monoamine NSS transporter substrate and ligand affinity. | Wang CI et al. | β | 2010 | β |
| Influence of ligand binding kinetics on functional inhibition of human recombinant serotonin and norepinephrine transporters. | Tsuruda PR et al. | β | 2010 | β |
| Modeling and dynamics of the inward-facing state of a Na+/Cl- dependent neurotransmitter transporter homologue. | Shaikh SA et al. | β | 2010 | β |
| Molecular dynamics of leucine and dopamine transporter proteins in a model cell membrane lipid bilayer. | Gedeon PC et al. | β | 2010 | β |
| Mutational mapping and modeling of the binding site for (S)-citalopram in the human serotonin transporter. | Andersen J et al. | β | 2010 | β |
| Receptor-Based Discovery of a Plasmalemmal Monoamine Transporter Inhibitor via High Throughput Docking and Pharmacophore Modeling. | Indarte M et al. | β | 2010 | β |
| Regulation of dopamine transporter function by protein-protein interactions: new discoveries and methodological challenges. | Eriksen J et al. | β | 2010 | β |
| Role of aberrant striatal dopamine D1 receptor/cAMP/protein kinase A/DARPP32 signaling in the paradoxical calming effect of amphetamine. | Napolitano F et al. | β | 2010 | β |
| Structural analysis of the extracellular entrance to the serotonin transporter permeation pathway. | Torres-Altoro MI et al. | β | 2010 | β |
| Structural perspectives on secondary active transporters. | Boudker O et al. | β | 2010 | β |
| Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters. | Zhang P et al. | β | 2010 | β |
| Substrate and drug binding sites in LeuT. | Nyola A et al. | β | 2010 | β |
| Syntaxin 1A regulates dopamine transporter activity, phosphorylation and surface expression. | Cervinski MA et al. | β | 2010 | β |
| The high-affinity binding site for tricyclic antidepressants resides in the outer vestibule of the serotonin transporter. | Sarker S et al. | β | 2010 | β |
| The high affinity dopamine uptake inhibitor, JHW 007, blocks cocaine-induced reward, locomotor stimulation and sensitization. | VelΓ‘zquez-SΓ‘nchez C et al. | β | 2010 | β |
| The novel triple reuptake inhibitor JZAD-IV-22 exhibits an antidepressant pharmacological profile without locomotor stimulant or sensitization properties. | Caldarone BJ et al. | β | 2010 | β |
| Transmembrane domain 6 of the human serotonin transporter contributes to an aqueously accessible binding pocket for serotonin and the psychostimulant 3,4-methylene dioxymethamphetamine. | Field JR et al. | β | 2010 | β |
| A dopamine transport inhibitor with markedly low abuse liability suppresses cocaine self-administration in the rat. | Ferragud A et al. | β | 2009 | β |
| An extended study of dimeric phenyl tropanes. | Nielsen S et al. | β | 2009 | β |
| Assessment of reinforcing effects of benztropine analogs and their effects on cocaine self-administration in rats: comparisons with monoamine uptake inhibitors. | Hiranita T et al. | β | 2009 | β |
| Combinations of cocaine with other dopamine uptake inhibitors: assessment of additivity. | Tanda G et al. | β | 2009 | β |
| Discovery of drugs to treat cocaine dependence: behavioral and neurochemical effects of atypical dopamine transport inhibitors. | Tanda G et al. | β | 2009 | β |
| Fluoxetine (Prozac) binding to serotonin transporter is modulated by chloride and conformational changes. | Tavoulari S et al. | β | 2009 | β |
| GABA transporter lysine 448: a key residue for tricyclic antidepressants interaction. | Cherubino F et al. | β | 2009 | β |
| Interaction of catechol and non-catechol substrates with externally or internally facing dopamine transporters. | Liang YJ et al. | β | 2009 | β |
| Ligand effects on cross-linking support a conformational mechanism for serotonin transport. | Tao Z et al. | β | 2009 | β |
| Location of the antidepressant binding site in the serotonin transporter: importance of Ser-438 in recognition of citalopram and tricyclic antidepressants. | Andersen J et al. | β | 2009 | β |
| Mechanism for cocaine blocking the transport of dopamine: insights from molecular modeling and dynamics simulations. | Huang X et al. | β | 2009 | β |
| Proline-directed phosphorylation of the dopamine transporter N-terminal domain. | Gorentla BK et al. | β | 2009 | β |
| Recent advances in the understanding of the interaction of antidepressant drugs with serotonin and norepinephrine transporters. | Andersen J et al. | β | 2009 | β |
| Recent progress in protein drug design and discovery with a focus on novel approaches to the development of anti-cocaine medications. | Zheng F et al. | β | 2009 | β |
| Review. The molecular logic of sodium-coupled neurotransmitter transporters. | Gouaux E | β | 2009 | β |
| The dopamine uptake inhibitor 3 alpha-[bis(4'-fluorophenyl)metoxy]-tropane reduces cocaine-induced early-gene expression, locomotor activity, and conditioned reward. | VelΓ‘zquez-SΓ‘nchez C et al. | β | 2009 | β |
| [Cocaine-binding site on the dopamine transporter clarified]. | Wenzel E et al. | β | 2008 | β |
| Interaction of cocaine-, benztropine-, and GBR12909-like compounds with wild-type and mutant human dopamine transporters: molecular features that differentially determine antagonist-binding properties. | Schmitt KC et al. | β | 2008 | β |