Antidepressant binding site in a bacterial homologue of neurotransmitter transporters

Nature

Volumn 448, Issue 7156, 2007, Pages 952-956

  Singh, Satinder K ^a   Yamashita, Atsuko ^b,c   Gouaux, Eric ^a  

^a OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

^b Howard Hughes Medical Institute Oregon Health and Science University ^*  (United States)

^c RIKEN SPring 8 Center   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDEPRESSANT AGENT; CLOMIPRAMINE; IMIPRAMINE; NEUROTRANSMITTER TRANSPORTER; SODIUM ION; TRICYCLIC ANTIDEPRESSANT AGENT;

BACTERIUM; EXPERIMENTAL DESIGN; GLUCOSE; ION; LIPID; MOLECULAR ANALYSIS; PROKARYOTE; PROTEIN; SODIUM;

ARTICLE; BINDING SITE; CRYSTAL STRUCTURE; HUMAN; LIPID BILAYER; PRIORITY JOURNAL; PROKARYOTIC CELL; REINFORCEMENT; STEADY STATE;

BACTERIA (MICROORGANISMS); HARNESS; MAMMALIA; PROKARYOTA;

EID: 34548178234     PISSN: 00280836     EISSN: 14764687     Source Type: Journal    
DOI: 10.1038/nature06038     Document Type: Article

References (30)

1. Hediger, M. A. et al. The ABCs of solute carriers: physiological, pathological and therapeutic implications of human membrane transport proteins. Introduction. Pflugers Arch. 447, 465-468 (2004).
2. Wright, E. M., Turk, E. & Martin, M. G. Molecular basis for glucose-galactose malabsorption. Cell Biochem. Biophys. 36, 115-121 (2002).
3. Pohlenz, J. & Refetoff, S. Mutations in the sodium/iodide symporter (NIS) gene as a cause for iodide transport defects and congenital hypothyroidism. Biochimie 81, 469-476 (1999).
4. Simon, D. B. et al. Gitelman's variant of Bartter's syndrome, inherited hypokalaemic alkalosis, is caused by mutations in the thiazide-sensitive Na-Cl cotransporter. Nature Genet. 12, 24-30 (1996).
5. Richerson, G. B. & Wu, Y. Role of the GABA transporter in epilepsy. Adv. Exp. Med. Biol. 548, 76-91 (2004).
6. Hahn, M. K. & Blakely, R. D. Monoamine transporter gene structure and polymorphisms in relation to psychiatric and other complex disorders. Pharmacogenomics J. 2, 217-235 (2002).
7. Sutcliffe, J. S. et al. Allelic heterogeneity at the serotonin transporter locus (SLC6A4) confers susceptibility to autism and rigid-compulsive behaviors. Am. J. Hum. Genet. 77, 265-279 (2005).
8. Ozaki, N. et al. Serotonin transporter missense mutation associated with a complex neuropsychiatric phenotype. Mol. Psychiatry 8, 933-936 (2003).
9. 3H]metolazone. Proc. Natl Acad. Sci. USA 85, 2311-2314 (1988).
10. Krogsgaard-Larsen, P., Frolund, B. & Frydenvang, K. GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Curr. Pharm. Des. 6, 1193-1209 (2000).
11. Barker, E. L. & Blakely, R. D. in Psychopharmacology - the Fourth Generation of Progress (eds Bloom, F. E. & Kupfer, D. J.) 321-333 (Raven, New York, 1995).
12. Talvenheimo, J., Nelson, P. J. & Rudnick, G. Mechanism of imipramine inhibition of platelet 5-hydroxytryptamine transport. J. Biol. Chem. 254, 4631-4635 (1979).
13. Smart, L. Competitive inhibition of sodium-dependent high affinity choline uptake by harmala alkaloids. Eur. J. Pharmacol. 75, 265-269 (1981).
14. - cotransporter of the thyroid: characterisation of new inhibitors. Pflugers Arch. 435, 259-266 (1998).
15. Uryu, K. et al. Inhibition by neuromuscular blocking drugs of norepinephrine transporter in cultured bovine adrenal medullary cells. Anesth. Analg. 91, 546-551 (2000).
16. Neubauer, H. A., Hansen, C. G. & Wiborg, O. Dissection of an allosteric mechanism on the serotonin transporter: a cross-species study. Mol. Pharmacol. 69, 1242-1250 (2006).
17. --dependent neurotransmitter transporters. Nature 437, 215-223 (2005).
18. --dependent neurotransmitter transporters: drugs, substrates, presynaptic receptors, and signaling systems. Pharmacol. Ther. 92, 21-55 (2001).
19. Cantu, M. D., Hillebranda, S. & Carrilho, E. Determination of the dissociation constants (pKa) of secondary and tertiary amines in organic media by capillary electrophoresis and their role in the electrophoretic mobility order inversion. J. Chromatogr. A. 1068, 99-105 (2005).
20. Zomot, E. & Kanner, B. I. The interaction of the c-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. J. Biol. Chem. 278, 42950-42958 (2003).
21. Norregaard, L., Frederiksen, D., Nielsen, E. O. & Gether, U. Delineation of an endogenous zinc-binding site in the human dopamine transporter. EMBO J. 17, 4266-4273 (1998).
22. 2+ inhibits glycine transport by glycine transporter subtype 1b. J. Biol. Chem. 279, 22983-22991 (2004).
23. 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. J. Biol. Chem. 279, 24089-24099 (2004).
24. Jardetzky, O. Simple allosteric model for membrane pumps. Nature 211, 969-970 (1966).
25. Zhang, Y. W. & Rudnick, G. The cytoplasmic substrate permeation pathway of serotonin transporter. J. Biol. Chem. 281, 36213-36220 (2006).
26. Keller, P. C. II, Stephan, M., Glomska, H. & Rudnick, G. Cysteine-scanning mutagenesis of the fifth external loop of serotonin transporter. Biochemistry 43, 8510-8516 (2004).
27. Henry, L. K., Adkins, E. M., Han, Q. & Blakely, R. D. Serotonin and cocaine-sensitive inactivation of human serotonin transporters by methanethiosulfonates targeted to transmembrane domain I. J. Biol. Chem. 278, 37052-37063 (2003).
28. Paczkowski, F. A., Sharpe, I. A., Dutertre, S. & Lewis, R. J. χ-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model. J. Biol. Chem. 282, 17837-17844 (2007).
29. Henry, L. K. et al. Tyr-95 and Ile-172 in transmembrane segments 1 and 3 of human serotonin transporters interact to establish high affinity recognition of antidepressants. J. Biol. Chem. 281, 2012-2023 (2006).
30. Kaplan, R. S. & Pedersen, P. L. Determination of microgram quantities of protein in the presence of milligram levels of lipid with amido black 10B. Anal. Biochem. 150, 97-104 (1985).