Species-scanning mutagenesis of the serotonin transporter reveals residues essential in selective, high-affinity recognition of antidepressants

Journal of Neurochemistry

Volumn 79, Issue 2, 2001, Pages 237-247

  Mortensen, Ole V ^a   Kristensen, Anders S ^a   Wiborg, Ove ^a  

^a AARHUS UNIVERSITY HOSPITAL   (Denmark)

Author keywords

Citalopram analogues; Cross species chimera

Indexed keywords

1 (3 DIMETHYLAMINOPROPAN 1 YL) 1 (4 FLUOROPHENYL) 1,3 DIHYDROBENZOISOFURAN; 3,4 METHYLENEDIOXYMETHAMPHETAMINE; 3BETA (4 IODOPHENYL) 2BETA TROPANECARBOXYLIC ACID METHYL ESTER; 5 CHLORO 1 (3 DIMETHYLAMINOPROPAN 1 YL) 1 (4 FLUOROPHENYL)BENZOISOFURAN; 5 CHLORO 1 (3 DIMETHYLAMINOPROPYL) 1 PHENYLPHTHALANOXALATE; 5 CYANO 1,3 DIHYDRO 1 (4 FLUOROPHENYL)ISOBENZOFURAN; ANTIDEPRESSANT AGENT; CITALOPRAM; COCAINE; COCAINE DERIVATIVE; FLUOXETINE; FLUVOXAMINE; IMIPRAMINE; LU 08052O; LU 09066C; LU 10134C; LU 11109C; LU 17046; METHIONINE; N METHYL 3 [5 CYANO 1 (4 FLUOROPHENYL)ISOBENZOFURAN 1 YL]PROPAN 1 YLAMINOXALATE; PAROXETINE; PHENYLALANINE; PSYCHOSTIMULANT AGENT; SEROTONIN TRANSPORTER; SERTRALINE; TYROSINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL STRAIN COS1; CHIMERA; CONTROLLED STUDY; DRUG PROTEIN BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; SEROTONIN UPTAKE;

ANIMALS; ANTIDEPRESSIVE AGENTS; ANTIDEPRESSIVE AGENTS, SECOND-GENERATION; CARRIER PROTEINS; CATTLE; CHIMERA; CITALOPRAM; COS CELLS; HUMANS; MEMBRANE GLYCOPROTEINS; MEMBRANE TRANSPORT PROTEINS; MUTAGENESIS, SITE-DIRECTED; NERVE TISSUE PROTEINS; SEROTONIN; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SEROTONIN UPTAKE INHIBITORS; SPECIES SPECIFICITY;

ANIMALIA; BOVINAE;

EID: 0034780661     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.2001.00587.x     Document Type: Article

References (30)

1. Identification of a single amino acid, phenylalanine 586, that is responsible for high affinity interactions of tricyclic antidepressants with the human serotonin transporter
2. 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
3. Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter
4. Cloning and expression of a functional serotonin transporter from rat brain
5. Tails of serotonin and norepinephrine transporters: Deletions and chimeras retain function
6. Amino acid residues that control pH modulation of transport-associated current in mammalian serotonin transporters
7. Cloning and expression of the mouse serotonin transporter
8. The third transmembrane domain of the serotonin transporter contains residues associated with substrate and cocaine binding
9. Determination of external loop topology in the serotonin transporter by site-directed chemical labeling
10. Guinea pig 5-HT transporter: Cloning, expression, distribution, and function in intestinal sensory reception
11. A cocaine-sensitive Drosophila serotonin transporter: Cloning, expression, and electrophysiological characterization
12. Cloning, expression, and localization of a chloride-facilitated, cocaine-sensitive serotonin transporter from Drosophila melanogaster
13. Serotonin uptake and serotonin uptake inhibition
14. A stereo-selective pharmacophoric model of the serotonin reuptake site
15. Cloning of a serotonin transporter affected by antidepressants
16. Isolation of a cDNA encoding the human brain serotonin transporter
17. Cation - Phi interactions in aromatics of biological and medicinal interest: Electrostatic potential surfaces as a useful qualitative guide
18. Restriction site-independent formation of chimeras from homologous neurotransmitter-transporter cDNAs
19. Molecular cloning, expression and characterization of a bovine serotonin transporter
20. The family of Na+/Cl- neurotransmitter transporters
21. Role of serotonin in the pathophysiology of depression: Focus on the serotonin transporter
22. Placental biogenic amine transporters: Cloning and expression
23. Antidepressant- and cocaine-sensitive human serotonin transporter: Molecular cloning, expression, and chromosomal localization
24. Phosphorylation and regulation of antidepressant-sensitive serotonin transporters
25. A new pharmophoric model for 5-HT reuptake-inhibitors: Differentiation of amphetamine analogues
26. An extracellular loop region of the serotonin transporter may be involved in the translocation mechanism
27. A single serine residue controls the cation dependence of substrate transport by the rat serotonin transporter
28. Three-dimensional structure of acetylcholinesterase and of its complexes with anticholinesterase drugs
29. Pharmacological profile of antidepressants and related compounds at human monoamine transporters
30. Cocaine and the serotonin saga