pubmed-article:17428804 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:17428804 | lifeskim:mentions | umls-concept:C0026336 | lld:lifeskim |
pubmed-article:17428804 | lifeskim:mentions | umls-concept:C0003290 | lld:lifeskim |
pubmed-article:17428804 | lifeskim:mentions | umls-concept:C0132800 | lld:lifeskim |
pubmed-article:17428804 | lifeskim:mentions | umls-concept:C0596902 | lld:lifeskim |
pubmed-article:17428804 | lifeskim:mentions | umls-concept:C1704675 | lld:lifeskim |
pubmed-article:17428804 | pubmed:issue | 24 | lld:pubmed |
pubmed-article:17428804 | pubmed:dateCreated | 2007-6-11 | lld:pubmed |
pubmed-article:17428804 | pubmed:abstractText | Monoamine neurotransmitter transporters for norepinephrine (NE), dopamine and serotonin are important targets for antidepressants and analgesics. The conopeptide chi-MrIA is a noncompetitive and highly selective inhibitor of the NE transporter (NET) and is being developed as a novel intrathecal analgesic. We used site-directed mutagenesis to generate a suite of mutated transporters to identify two amino acids (Leu(469) and Glu(382)) that affected the affinity of chi-MrIA to inhibit [(3)H]NE uptake through human NET. Residues that increased the K(d) of a tricyclic antidepressant (nisoxetine) were also identified (Phe(207), Ser(225), His(296), Thr(381), and Asp(473)). Phe(207), Ser(225), His(296), and Thr(381) also affected the rate of NE transport without affecting NE K(m). In a new model of NET constructed from the bLeuT crystal structure, chi-MrIA-interacting residues were located at the mouth of the transporter near residues affecting the binding of small molecule inhibitors. | lld:pubmed |
pubmed-article:17428804 | pubmed:language | eng | lld:pubmed |
pubmed-article:17428804 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17428804 | pubmed:citationSubset | IM | lld:pubmed |
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pubmed-article:17428804 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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pubmed-article:17428804 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17428804 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17428804 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17428804 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17428804 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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pubmed-article:17428804 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:17428804 | pubmed:month | Jun | lld:pubmed |
pubmed-article:17428804 | pubmed:issn | 0021-9258 | lld:pubmed |
pubmed-article:17428804 | pubmed:author | pubmed-author:LewisRichard... | lld:pubmed |
pubmed-article:17428804 | pubmed:author | pubmed-author:PaczkowskiFil... | lld:pubmed |
pubmed-article:17428804 | pubmed:author | pubmed-author:DutertreSébas... | lld:pubmed |
pubmed-article:17428804 | pubmed:author | pubmed-author:SharpeIain... | lld:pubmed |
pubmed-article:17428804 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:17428804 | pubmed:day | 15 | lld:pubmed |
pubmed-article:17428804 | pubmed:volume | 282 | lld:pubmed |
pubmed-article:17428804 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:17428804 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:17428804 | pubmed:pagination | 17837-44 | lld:pubmed |
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pubmed-article:17428804 | pubmed:year | 2007 | lld:pubmed |
pubmed-article:17428804 | pubmed:articleTitle | chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model. | lld:pubmed |
pubmed-article:17428804 | pubmed:affiliation | Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland 4072, Australia. | lld:pubmed |
pubmed-article:17428804 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:17428804 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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