Dissection of an allosteric mechanism on the serotonin transporter: A cross-species study

Molecular Pharmacology

Volumn 69, Issue 4, 2006, Pages 1242-1250

  Neubauer, Henrik Amtoft ^a   Hansen, Carsten Gram ^a   Wiborg, Ove ^a  

^a AARHUS UNIVERSITY HOSPITAL   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

3BETA (4 IODOPHENYL) 2BETA TROPANECARBOXYLIC ACID METHYL ESTER; CITALOPRAM; DULOXETINE; FLUOXETINE; SEROTONIN; SEROTONIN ANTAGONIST; SEROTONIN TRANSPORTER;

ALLOSTERISM; AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; CARBOXY TERMINAL SEQUENCE; CHIMERA; DRUG BINDING SITE; DRUG INHIBITION; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; MUTAGENESIS; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY;

ALLOSTERIC REGULATION; ANIMALS; CERCOPITHECUS AETHIOPS; CHICKENS; CHIMERA; CITALOPRAM; COS CELLS; MUTAGENESIS, SITE-DIRECTED; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SPECIES SPECIFICITY;

EID: 33645104973     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.105.018507     Document Type: Article

References (25)

1. Barker EL and Blakely RD (1995) in Psychopharmacology: The Fourth Generation of Progress (Bloom FE and Kupfer DJ eds) pp 321-333, Raven Press, New York.
2. Bunin MA and Wightman RM (1998) Quantitative evaluation of 5-hydroxytryptamine (serotonin) neuronal release and uptake: an investigation of extrasynaptic transmission. J Neurosci 18:4854-4860.
3. Chen F, Larsen MB, Neubauer HA, Sanchez C, Plenge P, and Wiborg O (2005a) Characterization of an allosteric citalopram-binding site at the serotonin transporter. J Neurochem 92:21-28.
4. Chen F, Larsen MB, Sanchez C, and Wiborg O (2005b) The S-enantiomer of R,S-citalopram increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors. Eur Neuropsychopharmacol 15:193-198.
5. Eisensamer B, Uhr M, Meyr S, Gimpl G, Deiml T, Rammes G, Lambert JJ, Zieglgansberger W, Holsboer F, and Rupprecht R (2005) Antidepressants and antipsychotic drugs colocalize with 5-HT3 receptors in raft-like domains. J Neurosci 25:10198-10206.
6. Hastrup H, Karlin A, and Javitch JA (2001) Symmetrical dimer of the human dopamine transporter revealed by cross-linking Cys-306 at the extracellular end of the sixth transmembrane segment. Proc Natl Acad Sci USA 98:10055-10060.
7. Hastrup H, Sen N, and Javitch JA (2003) 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. J Biol Chem 278:45045-45048.
8. Just H, Sitte HH, Schmid JA, Freissmuth M, and Kudlacek O (2004) Identification of an additional interaction domain in transmembrane domains 11 and 12 that supports oligomer formation in the human serotonin transporter. J Biol Chem 279:6650-6657.
9. Keller PC, Stephan M, Glomska H, and Rudnick G (2004) Cysteine-scanning mutagenesis of the fifth external loop of serotonin transporter. Biochemistry 43:8510-8516.
10. Kilic F and Rudnick G (2000) Oligomerization of serotonin transporter and its functional consequences. Proc Natl Acad Sci USA 97:3106-3111.
11. Kirsch RD and Joly E (1998) An improved PCR-mutagenesis strategy for two-site mutagenesis or sequence swapping between related genes. Nucleic Acids Res 26:1848-1850.
12. Larsen MB, Elfving B, and Wiborg O (2004) The chicken serotonin transporter discriminates between serotonin-selective reuptake inhibitors. A species-scanning mutagenesis study. J Biol Chem 279:42147-42156.
13. Magnani F, Tate CG, Wynne S, Williams C, and Haase J (2004) Partitioning of the serotonin transporter into lipid microdomains modulates transport of serotonin. J Biol Chem 279:38770-38778.
14. Mortensen OV, Kristensen AS, and Wiborg O (2001) Species-scanning mutagenesis of the serotonin transporter reveals residues essential in selective, high-affinity recognition of antidepressants. J Neurochem 79:237-247.
15. Owens MJ, Morgan WN, Plott SJ, and Nemeroff CB (1997) Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites. J Pharmacol Exp Ther 283:1305-1322.
16. 3H]paroxetine binding to platelet and neuronal membranes. Eur J Pharmacol 119:1-8.
17. Plenge P and Mellerup ET (1997) An affinity-modulating site on neuronal monoamine transport proteins. Pharmacol Toxicol 80:197-201.
18. 3H] citalopram binding to the 5-HT transporter from brain and platelets. Eur J Pharmacol 206:243-250.
19. Sur C, Betz H, and Schloss P (1997) A single serine residue controls the cation dependence of substrate transport by the rat serotonin transporter. Proc Natl Acad Sci USA 94:7639-7644.
20. Tatsumi M, Groshan K, Blakely RD, and Richelson E (1997) Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol 340:249-258.
21. 3H]imipramine from human platelet recognition sites. Eur J Pharmacol 86:303-307.
22. Wennogle LP and Meyerson LR (1985) Serotonin uptake inhibitors differentially modulate high affinity imipramine dissociation in human platelet membranes. Life Sci 36:1541-1550.
23. --dependent neurotransmitter transporters. Nature (Lond) 437:215-223.
24. Zhu CB, Hewlett WA, Feoktistov I, Biaggioni I, and Blakely RD (2004a) Adenosine receptor, protein kinase G and p38 mitogen-activated protein kinase-dependent up-regulation of serotonin transporters involves both transporter trafficking and activation. Mol Pharmacol 65:1462-1474.
25. Zhu CB, Hewlett WA, Francis SH, Corbin JD, and Blakely RD (2004b) Stimulation of serotonin transport by the cyclic GMP phosphodiesterase-5 inhibitor sildenafil. Eur J Pharmacol 504:1-6.