Emerging structure-function relationships defining monoamine NSS transporter substrate and ligand affinity

Biochemical Pharmacology

Volumn 79, Issue 8, 2010, Pages 1083-1091

  Wang, Ching I Anderson ^a   Lewis, Richard J ^a  

^a UNIVERSITY OF QUEENSLAND   (Australia)

Author keywords

Homology models; Leucine transporter; Monoamine transporter; Na+ Cl binding sites; Structure function relationship; Trafficking; Tricyclic antidepressant

Indexed keywords

4 AMINOBUTYRIC ACID CARRIER; ALANINE; AMINO ACID TRANSPORTER; ASPARTIC ACID; CARRIER PROTEIN; CLOMIPRAMINE; DESIPRAMINE; DOPAMINE; DOPAMINE TRANSPORTER; FLUOXETINE; GLUTAMATE TRANSPORTER; GLYCINE; GLYCINE TRANSPORTER; LEUCINE TRANSPORTER; MONOAMINE OXIDASE INHIBITOR; MONOAMINE TRANSPORTER; NEUROTRANSMITTER SODIUM COTRANSPORTER; NORADRENALIN; NORADRENALIN TRANSPORTER; PHENYLALANINE; SEROTONIN; SEROTONIN NORADRENALIN REUPTAKE INHIBITOR; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; SERTRALINE; TRICYCLIC ANTIDEPRESSANT AGENT; TRYPTOPHAN; TYROSINE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALINE;

ACCURACY; AMINO ACID SUBSTITUTION; ANXIETY DISORDER; AQUIFEX AEOLICUS; BINDING AFFINITY; BINDING SITE; BULIMIA; CRYSTAL STRUCTURE; DEPRESSION; DIARRHEA; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG SPECIFICITY; DRUG STRUCTURE; ENZYME SUBSTRATE; HEADACHE; HUMAN; INSOMNIA; LIGAND BINDING; MEDICAL RESEARCH; MOLECULAR INTERACTION; MUTATIONAL ANALYSIS; NONHUMAN; NOTE; PREDICTION; PREMENSTRUAL DYSPHORIC DISORDER; PRIORITY JOURNAL; PROTEIN FAMILY; PROTEIN FUNCTION; PROTEIN STRUCTURE; SEQUENCE ALIGNMENT; SEQUENCE HOMOLOGY; SEXUAL DYSFUNCTION; STRUCTURE ACTIVITY RELATION; SYNAPSE; TREMOR;

AMINO ACID SEQUENCE; ANIMALS; ANTIDEPRESSIVE AGENTS, TRICYCLIC; CRYSTALLIZATION; DOPAMINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; LEUCINE; LIGANDS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; NOREPINEPHRINE PLASMA MEMBRANE TRANSPORT PROTEINS; PROTEIN FOLDING; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SEROTONIN UPTAKE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 77249090654     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2009.11.019     Document Type: Note

References (118)

1. Masson J., Sagne C., Hamon M., El Mestikawy S. Neurotransmitter transporters in the central nervous system. Pharmacological Reviews 1999, 51:439-464.
2. Chen N.H., Reith M.E., Quick M.W. Synaptic uptake and beyond: the sodium- and chloride-dependent neurotransmitter transporter family SLC6. Pflugers Archiv 2004, 447:519-531.
3. Kanai Y., Hediger M.A. The glutamate/neutral amino acid transporter family SLC1: molecular, physiological and pharmacological aspects. Pflugers Archiv 2004, 447:469-479.
4. Guastella J., Nelson N., Nelson H., Czyzyk L., Keynan S., Miedel M.C., et al. Cloning and expression of a rat brain GABA transporter. Science (New York, NY) 1990, 249:1303-1306.
5. Chen J.G., Liu-Chen S., Rudnick G. Determination of external loop topology in the serotonin transporter by site-directed chemical labeling. The Journal of Biological Chemistry 1998, 273:12675-12681.
6. Veenhoff L.M., Heuberger E.H., Poolman B. Quaternary structure and function of transport proteins. Trends in Biochemical Sciences 2002, 27:242-249.
7. Kilic F., Rudnick G. Oligomerization of serotonin transporter and its functional consequences. Proceedings of the National Academy of Sciences of the United States of America 2000, 97:3106-3111.
8. Chang A.S., Starnes D.M., Chang S.M. Possible existence of quaternary structure in the high-affinity serotonin transport complex. Biochemical and Biophysical Research Communications 1998, 249:416-421.
9. Schmid J.A., Scholze P., Kudlacek O., Freissmuth M., Singer E.A., Sitte H.H. Oligomerization of the human serotonin transporter and of the rat GABA transporter 1 visualized by fluorescence resonance energy transfer microscopy in living cells. The Journal of Biological Chemistry 2001, 276:3805-3810.
10. Torres G.E., Carneiro A., Seamans K., Fiorentini C., Sweeney A., Yao W.D., et al. Oligomerization and trafficking of the human dopamine transporter. Mutational analysis identifies critical domains important for the functional expression of the transporter. The Journal of Biological Chemistry 2003, 278:2731-2739.
11. Hastrup H., Karlin A., Javitch J.A. Symmetrical dimer of the human dopamine transporter revealed by cross-linking Cys-306 at the extracellular end of the sixth transmembrane segment. Proceedings of the National Academy of Sciences of the United States of America 2001, 98:10055-10060.
12. Hastrup H., Sen N., Javitch J.A. The human dopamine transporter forms a tetramer in the plasma membrane: cross-linking of a cysteine in the fourth transmembrane segment is sensitive to cocaine analogs. The Journal of Biological Chemistry 2003, 278:45045-45048.
13. Scholze P., Freissmuth M., Sitte H.H. Mutations within an intramembrane leucine heptad repeat disrupt oligomer formation of the rat GABA transporter 1. The Journal of Biological Chemistry 2002, 277:43682-43690.
14. Klingenberg M. Membrane protein oligomeric structure and transport function. Nature 1981, 290:449-454.
15. Nguyen T.T., Amara S.G. N-linked oligosaccharides are required for cell surface expression of the norepinephrine transporter but do not influence substrate or inhibitor recognition. Journal of Neurochemistry 1996, 67:645-655.
16. Tate C.G., Blakely R.D. The effect of N-linked glycosylation on activity of the Na(+)- and Cl(-)-dependent serotonin transporter expressed using recombinant baculovirus in insect cells. The Journal of Biological Chemistry 1994, 269:26303-26310.
17. Melikian H.E., Ramamoorthy S., Tate C.G., Blakely R.D. Inability to N-glycosylate the human norepinephrine transporter reduces protein stability, surface trafficking, and transport activity but not ligand recognition. Molecular Pharmacology 1996, 50:266-276.
18. Chang M.Y., Lee S.H., Kim J.H., Lee K.H., Kim Y.S., Son H., et al. Protein kinase C-mediated functional regulation of dopamine transporter is not achieved by direct phosphorylation of the dopamine transporter protein. Journal of Neurochemistry 2001, 77:754-761.
19. Sakai N., Sasaki K., Nakashita M., Honda S., Ikegaki N., Saito N. Modulation of serotonin transporter activity by a protein kinase C activator and an inhibitor of type 1 and 2A serine/threonine phosphatases. Journal of Neurochemistry 1997, 68:2618-2624.
20. Foster J.D., Pananusorn B., Vaughan R.A. Dopamine transporters are phosphorylated on N-terminal serines in rat striatum. The Journal of Biological Chemistry 2002, 277:25178-25186.
21. Ritz M.C., Lamb R.J., Goldberg S.R., Kuhar M.J. Cocaine receptors on dopamine transporters are related to self-administration of cocaine. Science (New York, NY) 1987, 237:1219-1223.
22. Amara S.G., Sonders M.S. Neurotransmitter transporters as molecular targets for addictive drugs. Drug and Alcohol Dependence 1998, 51:87-96.
23. Hahn M.K., Robertson D., Blakely R.D. A mutation in the human norepinephrine transporter gene (SLC6A2) associated with orthostatic intolerance disrupts surface expression of mutant and wild-type transporters. The Journal of Neuroscience 2003, 23:4470-4478.
24. Hahn M.K., Blakely R.D. Monoamine transporter gene structure and polymorphisms in relation to psychiatric and other complex disorders. The Pharmacogenomics Journal 2002, 2:217-235.
25. Richerson G.B., Wu Y. Role of the GABA transporter in epilepsy. Advances in Experimental Medicine and Biology 2004, 548:76-91.
26. Kilic F., Murphy D.L., Rudnick G. A human serotonin transporter mutation causes constitutive activation of transport activity. Molecular Pharmacology 2003, 64:440-446.
27. Sutcliffe J.S., Delahanty R.J., Prasad H.C., McCauley J.L., Han Q., Jiang L., et al. Allelic heterogeneity at the serotonin transporter locus (SLC6A4) confers susceptibility to autism and rigid-compulsive behaviors. American Journal of Human Genetics 2005, 77:265-279.
28. Giros B., Jaber M., Jones S.R., Wightman R.M., Caron M.G. Hyperlocomotion and indifference to cocaine and amphetamine in mice lacking the dopamine transporter. Nature 1996, 379:606-612.
29. Xu F., Gainetdinov R.R., Wetsel W.C., Jones S.R., Bohn L.M., Miller G.W., et al. Mice lacking the norepinephrine transporter are supersensitive to psychostimulants. Nature Neuroscience 2000, 3:465-471.
30. Bengel D., Murphy D.L., Andrews A.M., Wichems C.H., Feltner D., Heils A., et al. Altered brain serotonin homeostasis and locomotor insensitivity to 3,4-methylenedioxymethamphetamine (" Ecstasy" ) in serotonin transporter-deficient mice. Molecular Pharmacology 1998, 53:649-655.
31. Kim H.J., Im J.H., Yang S.O., Moon D.H., Ryu J.S., Bong J.K., et al. Imaging and quantitation of dopamine transporters with iodine-123-IPT in normal and Parkinson's disease subjects. Journal of Nuclear Medicine 1997, 38:1703-1711.
32. Jeon B., Kim J.M., Jeong J.M., Kim K.M., Chang Y.S., Lee D.S., et al. Dopamine transporter imaging with [123I]-beta-CIT demonstrates presynaptic nigrostriatal dopaminergic damage in Wilson's disease. Journal of Neurology, Neurosurgery, and Psychiatry 1998, 65:60-64.
33. Wong D.F., Harris J.C., Naidu S., Yokoi F., Marenco S., Dannals R.F., et al. Dopamine transporters are markedly reduced in Lesch-Nyhan disease in vivo. Proceedings of the National Academy of Sciences of the United States of America 1996, 93:5539-5543.
34. Dougherty D.D., Bonab A.A., Spencer T.J., Rauch S.L., Madras B.K., Fischman A.J. Dopamine transporter density in patients with attention deficit hyperactivity disorder. Lancet 1999, 354:2132-2133.
35. Klimek V., Stockmeier C., Overholser J., Meltzer H.Y., Kalka S., Dilley G., et al. Reduced levels of norepinephrine transporters in the locus coeruleus in major depression. The Journal of Neuroscience 1997, 17:8451-8458.
36. Tiihonen J., Kuikka J.T., Bergstrom K.A., Karhu J., Viinamaki H., Lehtonen J., et al. Single-photon emission tomography imaging of monoamine transporters in impulsive violent behaviour. European Journal of Nuclear Medicine 1997, 24:1253-1260.
37. --dependent neurotransmitter transporters. Nature 2005, 437:215-223.
38. Singh S.K., Yamashita A., Gouaux E. Antidepressant binding site in a bacterial homologue of neurotransmitter transporters. Nature 2007, 448:952-956.
39. Zhou Z., Zhen J., Karpowich N.K., Law C.J., Reith M.E., Wang D.N. Antidepressant specificity of serotonin transporter suggested by three LeuT-SSRI structures. Nature Structural & Molecular Biology 2009.
40. Delgado P.L. How antidepressants help depression: mechanisms of action and clinical response. The Journal of Clinical Psychiatry 2004, 65(Suppl. 4):25-30.
41. Duman R.S., Heninger G.R., Nestler E.J. A molecular and cellular theory of depression. Archives of General Psychiatry 1997, 54:597-606.
42. Schildkraut J.J. The catecholamine hypothesis of affective disorders: a review of supporting evidence. The American Journal of Psychiatry 1965, 122:509-522.
43. Duman R.S., Monteggia L.M. A neurotrophic model for stress-related mood disorders. Biological Psychiatry 2006, 59:1116-1127.
44. Iversen L.L., Glennon R.A. Antidepressants. Chemistry BsM 2003, 483-524. Wiley, New York. D.J. Abraham (Ed.).
45. Olfson M., Marcus S.C., Druss B., Elinson L., Tanielian T., Pincus H.A. National trends in the outpatient treatment of depression. The Journal of the American Medical Association 2002, 287:203-209.
46. Buckley N.A., McManus P.R. Fatal toxicity of serotoninergic and other antidepressant drugs: analysis of United Kingdom mortality data. BMJ 2002, 325:1332-1333. (Clinical Research ed).
47. Thase M.E., Kupfer D.J. Recent developments in the pharmacotherapy of mood disorders. Journal of Consulting and Clinical Psychology 1996, 64:646-659.
48. Kennedy S.H., Andersen H.F., Lam R.W. Efficacy of escitalopram in the treatment of major depressive disorder compared with conventional selective serotonin reuptake inhibitors and venlafaxine XR: a meta-analysis. Journal of Psychiatry & Neuroscience 2006, 31:122-131.
49. Preskorn S.H. Comparison of the tolerability of bupropion, fluoxetine, imipramine, nefazodone, paroxetine, sertraline, and venlafaxine. The Journal of Clinical Psychiatry 1995, 56(Suppl. 6):12-21.
50. + antiporter and insights into mechanism of action and regulation by pH. Nature 2005, 435:1197-1202.
51. Adkins E.M., Barker E.L., Blakely R.D. Interactions of tryptamine derivatives with serotonin transporter species variants implicate transmembrane domain I in substrate recognition. Molecular Pharmacology 2001, 59:514-523.
52. Barker E.L., Perlman M.A., Adkins E.M., Houlihan W.J., Pristupa Z.B., Niznik H.B., et al. High affinity recognition of serotonin transporter antagonists defined by species-scanning mutagenesis. An aromatic residue in transmembrane domain I dictates species-selective recognition of citalopram and mazindol. The Journal of Biological Chemistry 1998, 273:19459-19468.
53. 2+ mobilization in antigen-stimulated mast cells. Journal of Leukocyte Biology 1999, 65:321-329.
54. Henry L.K., Defelice L.J., Blakely R.D. Getting the message across: a recent transporter structure shows the way. Neuron 2006, 49:791-796.
55. Kitayama S., Shimada S., Xu H., Markham L., Donovan D.M., Uhl G.R. Dopamine transporter site-directed mutations differentially alter substrate transport and cocaine binding. Proceedings of the National Academy of Sciences of the United States of America 1992, 89:7782-7785.
56. + transport. Synapse (New York, NY) 1993, 15:58-62.
57. Kristensen A.S., Larsen M.B., Johnsen L.B., Wiborg O. Mutational scanning of the human serotonin transporter reveals fast translocating serotonin transporter mutants. The European Journal of Neuroscience 2004, 19:1513-1523.
58. Lin Z., Wang W., Kopajtic T., Revay R.S., Uhl G.R. Dopamine transporter: transmembrane phenylalanine mutations can selectively influence dopamine uptake and cocaine analog recognition. Molecular Pharmacology 1999, 56:434-447.
59. Mitsuhata C., Kitayama S., Morita K., Vandenbergh D., Uhl G.R., Dohi T. Tyrosine-533 of rat dopamine transporter: involvement in interactions with 1-methyl-4-phenylpyridinium and cocaine. Brain Research 1998, 56:84-88.
60. Penado K.M., Rudnick G., Stephan M.M. Critical amino acid residues in transmembrane span 7 of the serotonin transporter identified by random mutagenesis. The Journal of Biological Chemistry 1998, 273:28098-28106.
61. Kitayama S., Morita K., Dohi T., Wang J.B., Davis S.C., Uhl G.R. Dissection of dopamine and cocaine binding sites on the rat dopamine transporter expressed in COS cells. Annals of the New York Academy of Sciences 1996, 801:388-393.
62. Ravna A.W. Three-dimensional models of neurotransmitter transporters and their interactions with cocaine and S-citalopram. The World Journal of Biological Psychiatry 2006, 7:99-109.
63. Ravna A.W., Edvardsen O. A putative three-dimensional arrangement of the human serotonin transporter transmembrane helices: a tool to aid experimental studies. Journal of Molecular Graphics & Modelling 2001, 20:133-144.
64. Ravna A.W., Sylte I., Dahl S.G. Molecular mechanism of citalopram and cocaine interactions with neurotransmitter transporters. The Journal of Pharmacology and Experimental Therapeutics 2003, 307:34-41.
65. Ravna A.W., Sylte I., Kristiansen K., Dahl S.G. Putative drug binding conformations of monoamine transporters. Bioorganic & Medicinal Chemistry 2006, 14:666-675.
66. Abramson J., Smirnova I., Kasho V., Verner G., Kaback H.R., Iwata S. Structure and mechanism of the lactose permease of Escherichia coli. Science (New York, NY) 2003, 301:610-615.
67. Fiser A., Sali A. Modeller: generation and refinement of homology-based protein structure models. Methods in Enzymology 2003, 374:461-491.
68. Chotia C., Lesk A. The relation between the divergence of sequence and structure in proteins. The EMBO Journal 1986, 5:823-826.
69. Altschul S.F., Madden T.L., Schaffer A.A., Zhang J.H., Zhang Z., Miller W., et al. Gapped BLAST and PSI-BLAST: a new generation of protein database search programs. Nucleic Acids Research 1997, 25:3389-3402.
70. + symporters (NSS) aids in the use of the LeuT structure to probe NSS structure and function. Molecular Pharmacology 2006, 70:1630-1642.
71. Huang X., Zhan C.G. How dopamine transporter interacts with dopamine: insights from molecular modeling and simulation. Biophysical Journal 2007, 93:3627-3639.
72. Indarte M., Madura J.D., Surratt C.K. Dopamine transporter comparative molecular modeling and binding site prediction using the LeuT(Aa) leucine transporter as a template. Proteins 2008, 70:1033-1046.
73. +/sugar symport. Science (New York, NY) 2008, 321:810-814.
74. Zhou Y., Zomot E., Kanner B.I. Identification of a lithium interaction site in the gamma-aminobutyric acid (GABA) transporter GAT-1. The Journal of Biological Chemistry 2006, 281:22092-22099.
75. Mager S., Naeve J., Quick M., Labarca C., Davidson N., Lester H.A. Steady states, charge movements, and rates for a cloned GABA transporter expressed in Xenopus oocytes. Neuron 1993, 10:177-188.
76. Mager S., Kleinberger-Doron N., Keshet G.I., Davidson N., Kanner B.I., Lester H.A. Ion binding and permeation at the GABA transporter GAT1. The Journal of Neuroscience 1996, 16:5405-5414.
77. Quick M., Yano H., Goldberg N.R., Duan L.H., Beuming T., Shi L., et al. State-dependent conformations of the translocation pathway in the tyrosine transporter Tyt1, a novel neurotransmitter: sodium symporter from Fusobacterium nucleatum. Journal of Biological Chemistry 2006, 281:26444-26454.
78. Rudnick G, Wall S.C. The molecular mechanism of " ecstasy" [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proceedings of the National Academy of Sciences of the United States of America 1992, 89:1817-1821.
79. Stephan M.M., Chen M.A., Penado K.M., Rudnick G. An extracellular loop region of the serotonin transporter may be involved in the translocation mechanism. Biochemistry 1997, 36:1322-1328.
80. Smicun Y., Campbell S.D., Chen M.A., Gu H., Rudnick G. The role of external loop regions in serotonin transport. Loop scanning mutagenesis of the serotonin transporter external domain. The Journal of Biological Chemistry 1999, 274:36058-36064.
81. +/Cl-dependent transporters. Proceedings of the National Academy of Sciences of the United States of America 2007, 104:12761-12766.
82. Zomot E., Bendahan A., Quick M., Zhao Y., Javitch J.A., Kanner B.I. Mechanism of chloride interaction with neurotransmitter:sodium symporters. Nature 2007, 449:726-730.
83. Erreger K., Grewer C., Javitch J.A., Galli A. Currents in response to rapid concentration jumps of amphetamine uncover novel aspects of human dopamine transporter function. The Journal of Neuroscience 2008, 28:976-989.
84. Tavoulari S., Forrest L.R., Rudnick G. Fluoxetine (Prozac) binding to serotonin transporter is modulated by chloride and conformational changes. The Journal of Neuroscience 2009, 29:9635-9643.
85. Zomot E., Kanner B.I. The interaction of the gamma-aminobutyric acid transporter GAT-1 with the neurotransmitter is selectively impaired by sulfhydryl modification of a conformationally sensitive cysteine residue engineered into extracellular loop IV. The Journal of Biological Chemistry 2003, 278:42950-42958.
86. Norregaard L., Frederiksen D., Nielsen E.O., Gether U. Delineation of an endogenous zinc-binding site in the human dopamine transporter. The EMBO Journal 1998, 17:4266-4273.
87. 2+ inhibits glycine transport by glycine transporter subtype 1b. The Journal of Biological Chemistry 2004, 279:22983-22991.
88. Mitchell S.M., Lee E., Garcia M.L., Stephan M.M. Structure and function of extracellular loop 4 of the serotonin transporter as revealed by cysteine-scanning mutagenesis. The Journal of Biological Chemistry 2004, 279:24089-24099.
89. Zhou Z., Zhen J., Karpowich N.K., Goetz R.M., Law C.J., Reith M.E., et al. LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake. Science (New York, NY) 2007, 317:1390-1393.
90. Talvenheimo J., Nelson P.J., Rudnick G. Mechanism of imipramine inhibition of platelet 5-hydroxytryptamine transport. The Journal of Biological Chemistry 1979, 254:4631-4635.
91. Apparsundaram S., Stockdale D.J., Henningsen R.A., Milla M.E., Martin R.S. Antidepressants targeting the serotonin reuptake transporter act via a competitive mechanism. The Journal of Pharmacology and Experimental Therapeutics 2008, 327:982-990.
92. Kimelberg H.K., Pelton E.W. High-affinity uptake of [3H]norepinephrine by primary astrocyte cultures and its inhibition by tricyclic antidepressants. Journal of Neurochemistry 1983, 40:1265-1270.
93. Chen J., Lu G., Lin J., Davidson A.L., Quiocho F.A. A tweezers-like motion of the ATP-binding cassette dimer in an ABC transport cycle. Molecular Cell 2003, 12:651-661.
94. Singh S.K., Piscitelli C.L., Yamashita A., Gouaux E. A competitive inhibitor traps LeuT in an open-to-out conformation. Science (New York, NY) 2008, 322:1655-1661.
95. Ravna A.W., Jaronczyk M., Sylte I. A homology model of SERT based on the LeuT(Aa) template. Bioorganic & Medicinal Chemistry Letters 2006, 16:5594-5597.
96. Dodd J.R., Christie D.L. Selective amino acid substitutions convert the creatine transporter to a gamma-aminobutyric acid transporter. The Journal of Biological Chemistry 2007, 282:15528-15533.
97. Beuming T., Kniazeff J., Bergmann M.L., Shi L., Gracia L., Raniszewska K., et al. The binding sites for cocaine and dopamine in the dopamine transporter overlap. Nature Neuroscience 2008, 11:780-789.
98. Forrest L.R., Zhang Y.W., Jacobs M.T., Gesmonde J., Xie L., Honig B.H., et al. Mechanism for alternating access in neurotransmitter transporters. Proceedings of the National Academy of Sciences of the United States of America 2008, 105:10338-10343.
99. Zhang Y.W., Rudnick G. The cytoplasmic substrate permeation pathway of serotonin transporter. The Journal of Biological Chemistry 2006, 281:36213-36220.
100. Jacobs M.T., Zhang Y.W., Campbell S.D., Rudnick G. Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter. The Journal of Biological Chemistry 2007, 282:29441-29447.
101. Celik L., Sinning S., Severinsen K., Hansen C.G., Moller M.S., Bols M., et al. Binding of serotonin to the human serotonin transporter. Molecular modeling and experimental validation. Journal of the American Chemical Society 2008, 130:3853-3865.
102. Lee S.H., Chang M.Y., Lee K.H., Park B.S., Lee Y.S., Chin H.R., et al. Importance of valine at position 152 for the substrate transport and 2beta-carbomethoxy-3beta-(4-fluorophenyl)tropane binding of dopamine transporter. Molecular Pharmacology 2000, 57:883-889.
103. Melamed N., Kanner B.I. Transmembrane domains I and II of the gamma-aminobutyric acid transporter GAT-4 contain molecular determinants of substrate specificity. Molecular Pharmacology 2004, 65:1452-1461.
104. Chen N.H., Reith M.E.A. Structure and function of the dopamine transporter. European Journal of Pharmacology 2000, 405:329-339.
105. Norregaard L., Gether U. The monoamine neurotransmitter transporters: structure, conformational changes and molecular gating. Current Opinion in Drug Discovery & Development 2001, 4:591-601.
106. Goldberg N.R., Beuming T., Soyer O.S., Goldstein R.A., Weinstein H., Javitch J.A. Probing conformational changes in neurotransmitter transporters: a structural context. European Journal of Pharmacology 2003, 479:3-12.
107. Volz T.J., Schenk J.O. A comprehensive atlas of the topography of functional groups of the dopamine transporter. Synapse (New York, NY) 2005, 58:72-94.
108. Wu X., Gu H.H. Cocaine affinity decreased by mutations of aromatic residue phenylalanine 105 in the transmembrane domain 2 of dopamine transporter. Molecular Pharmacology 2003, 63:653-658.
109. Gu H.H., Wu X., Han D.D. Conserved serine residues in serotonin transporter contribute to high-affinity cocaine binding. Biochemical and Biophysical Research Communications 2006, 343:1179-1185.
110. Neubauer H.A., Hansen C.G., Wiborg O. Dissection of an allosteric mechanism on the serotonin transporter: a cross-species study. Molecular Pharmacology 2006, 69:1242-1250.
111. Sucic S., Bryan-Lluka L.J. The role of the conserved GXXXRXG motif in the expression and function of the human norepinephrine transporter. Brain Research 2002, 108:40-50.
112. Zhang Y.W., Rudnick G. Cysteine-scanning mutagenesis of serotonin transporter intracellular loop 2 suggests an alpha-helical conformation. Journal of Biological Chemistry 2005, 280:30807-30813.
113. Androutsellis-Theotokis A., Goldberg N.R., Ueda K., Beppu T., Beckman M.L., Das S., et al. Characterization of a functional bacterial homologue of sodium-dependent neurotransmitter transporters. Journal of Biological Chemistry 2003, 278:12703-12709.
114. Andersen J., Kristensen A.S., Bang-Andersen B., Stromgaard K. Recent advances in the understanding of the interaction of antidepressant drugs with serotonin and norepinephrine transporters. Chemical Communications (Cambridge, England) 2009, 3677-3692.
115. + and substrate is triggered by substrate in a second binding site. Molecular Cell 2008, 30:667-677.
116. Paczkowski F.A., Sharpe I.A., Dutertre S. Lewis RJ. chi-conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model. Journal of Biological Chemistry 2007, 282:17837-17844.
117. Giros B., Wang Y.M., Suter S., McLeskey S.B., Pifl C., Caron M.G. Delineation of discrete domains for substrate, cocaine, and tricyclic antidepressant interactions using chimeric dopamine-norepinephrine transporters. The Journal of Biological Chemistry 1994, 269:15985-15988.
118. Larkin M.A., Blackshields G., Brown N.P., Chenna R., McGettigan P.A., McWilliam H., et al. ClustalW and ClustalX version 2. Bioinformatics 2007, 23:2947-2948.