Conformational flexibility of transmembrane helix VII of the human serotonin transporter impacts ion dependence and transport

Biochemical Pharmacology

Volumn 80, Issue 9, 2010, Pages 1418-1426

  Wenthur, Cody J ^a   Rodríguez, Gustavo J ^a   Kuntz, Charles P ^a   Barker, Eric L ^a  

^a PURDUE UNIVERSITY   (United States)

Author keywords

Amphetamine; Biogenic amine; Cocaine; Protein structure

Indexed keywords

3,4 DICHLOROAMPHETAMINE; 3BETA (4 IODOPHENYL) 2BETA TROPANECARBOXYLIC ACID METHYL ESTER; 5 METHOXY 6 METHYL 2 AMINOINDAN; [2 (TRIMETHYLAMMONIUM)ETHYL]METHANETHIOSULFONATE; AMPHETAMINE DERIVATIVE; CARRIER PROTEIN; CHLORIDE; CITALOPRAM; CYSTEINE; FLUOXETINE; IMIPRAMINE; INDAN DERIVATIVE; LEUCINE; SEROTONIN; SEROTONIN TRANSPORTER; SERTRALINE; SODIUM; SULFONE DERIVATIVE; TRANSMEMBRANE HELIX 7; TRITIUM; UNCLASSIFIED DRUG; VENLAFAXINE; 1 METHYL 4 PHENYLPYRIDINIUM;

AQUIFEX AEOLICUS; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DROSOPHILA; GENE MUTATION; GENETIC IDENTIFICATION; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN TRANSPORT; CELL CULTURE; CHEMICAL STRUCTURE; CHEMISTRY; HUMAN; METABOLISM; PHYSIOLOGY; PROTEIN SECONDARY STRUCTURE; STRUCTURE ACTIVITY RELATION; TRANSPORT AT THE CELLULAR LEVEL;

1-METHYL-4-PHENYLPYRIDINIUM; BIOLOGICAL TRANSPORT; CELLS, CULTURED; CHLORIDES; HUMANS; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN STRUCTURE, SECONDARY; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SODIUM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77956648298     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2010.07.005     Document Type: Article

References (25)

1. Jacobs B.L., Fornal C.A. Serotonin and behavior: a general hypothesis. Psychopharmacology: The Fourth Generation of Progress 1995, 461-469. Raven Press, New York. F. Bloom, D. Kupfer (Eds.).
2. Rudnick G., Wall S.C. p-Chloroamphetamine induces serotonin release through serotonin transporters. Biochemistry 1992, 31:6710-6718.
3. Rudnick G., Wall S.C. The molecular mechanism of " ecstasy": serotonin transporters are targets for MDMA-induced serotonin release. Proc. Natl. Acad. Sci. U.S.A. 1992, 89:1817-1821.
4. Wall S.C., Gu H., Rudnick G. Biogenic amine flux mediated by cloned transporters stably expressed in cultured cell lines: amphetamine specificity for inhibition and efflux. Mol. Pharmacol. 1995, 47:544-550.
5. Blakely R.D., Berson H.E., Fremeau R.T.J., Caron M.G., Peek M.M., Prince H.K., et al. Cloning and expression of a functional serotonin transporter from rat brain. Nature 1991, 354:66-70.
6. Hoffman B.J., Mezey E., Brownstein M.J. Cloning of a serotonin transporter affected by antidepressants. Science 1991, 254:579-580.
7. Ramamoorthy S., Bauman A.L., Moore K.R., Han H., Yang Feng T., Chang A.S., et al. Antidepressant- and cocaine-sensitive human serotonin transporter: molecular cloning, expression, and chromosomal localization. Proc. Natl. Acad. Sci. U.S.A. 1993, 90:2542-2546.
8. Demchyshyn L.L., Pristupa Z.B., Sugamori K.S., Barker E.L., Blakely R.D., Wolfgang W.J., et al. Cloning, expression, and localization of a chloride-facilitated cocaine-sensitive serotonin transporter from Drosophila melanogaster. Proc. Natl. Acad. Sci. U.S.A. 1994, 91:5158-5162.
9. Yamashita A., Singh S.K., Kawate T., Jin Y., Gouaux E. Crystal structure of a bacterial homologue of Na+/Cl--dependent neurotransmitter transporters. Nature 2005, 437:203-205.
10. Beuming T., Shi L., Javitch J.A., Weinstein H. A comprehensive structure-based alignment of prokaryotic and eukaryotic neurotransmitter/Na+ symporters (NSS) aids in the use of the LeuT structure to probe NSS structure and function. Mol. Pharmacol. 2006, 70:1630-1642.
11. White K.J., Kiser P.D., Nichols D.E., Barker E.L. Engineered zinc-binding sites confirm proximity and orientation of transmembrane helices I and III in the human serotonin transporter. Protein Sci. 2006, 15:2411-2422.
12. 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. Proc. Natl. Acad. Sci. U.S.A. 1992, 89:7782-7785.
13. Penado K.M.Y., Rudnick G., Stephan M.M. Critical amino acid residues in transmembrane Span 7 of the serotonin transporter identified by random mutagenesis. J. Biol. Chem. 1998, 273:28098-28106.
14. 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.
15. Forrest L.R., Tavoulari S., Zhang Y.W., Rudnick G., Honig B. Identification of a chloride ion binding site in Na+/Cl-dependent transporters. Proc. Natl. Acad. Sci. U.S.A. 2007, 104:12761-12766.
16. Kamdar G., Penado K.M.Y., Rudnick G., Stephan M.M. Functional role of critical stripe residues in transmembrane Span 7 of the serotonin transporter. J. Biol. Chem. 2001, 276:4038-4045.
17. Rodriguez G.J., Roman D.L., White K.J., Nichols D.E., Barker E.L. Distinct recognition of substrates by the human and Drosophila serotonin transporters. J. Pharmacol. Exp. Ther. 2003, 306:338-346.
18. Roman D.L., Walline C.C., Rodriguez G.J., Barker E.L. Interactions of antidepressants with the serotonin transporter: a contemporary molecular analysis. Eur. J. Pharmacol. 2003, 479:53-63.
19. Chen J.G., Liu-Chen S., Rudnick G. External cysteine residues in the serotonin transporter. Biochemistry 1997, 36:1479-1486.
20. Norregaard L., Loland C.J., Gether U. Evidence for distinct sodium-, dopamine-, and cocaine-dependent conformational changes in transmembrane segment 7 and 8 of the dopamine transporter. J. Biol. Chem. 2003, 278:30587-30596.
21. Fiser A., Sali A. Modeller: generation and refinement of homology-based protein structure models. Method Enzymol. 2003, 374:461-491.
22. Shen M.Y., Sali A. Statistical potential for assessment and prediction of protein structures. Protein Sci. 2006, 15:2507-2524.
23. Morris G.M., Huey R., Lindstrom W., Sanner M.F., Belew R.K., Goodsell D.S., et al. AutoDock4 and AutoDockTools4: automated docking with selective receptor flexibility. J. Comp. Chem. 2009, 16:2785-2791.
24. Van Der Spoel D., Lindahl E., Hess B., Groenhof G., Mark A., Berendsen J.C. GROMACS: fast, flexible, and free. J. Comp. Chem. 2005, 16:1701-1718.
25. Ni Y.G., Chen J.-G., Androutsellis-Theotokis A., Huang C.-J., Moczydlowski E., Rudnick G. A lithium-induced conformational change in serotonin transporter alters cocaine binding, ion conductance, and reactivity of Cys-109. J. Biol. Chem. 2001, 276:30942-30947.