Antagonist-induced conformational changes in dopamine transporter extracellular loop two involve residues in a potential salt bridge
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- 作者：Jon D. Gaffaney ; Madhur Shetty ; Bruce Felts ; Akula-Bala Pramod ; James D. Foster ; L. Keith Henry ; keith.henry@med.und.edu" class="auth_mail ; Roxanne A. Vaughan ; roxanne.vaughan@med.und.edu" class="auth_mail
- 关键词：DAT ; dopamine transporter ; NET ; norepinephrine transporter ; SERT ; serotonin transporter ; TM ; transmembrane domain ; EL ; extracellular loop ; IL ; intracellular loop ; o.w.w. ; original wet weight ; BCIP/NBT ; 5-bromo-4-chloro-3-indolyl phosphate/nitro blue ; CFT ; 2尾-carbomethoxy-3尾-(4-flourophenyl)tropane ; GBR12909 ; [2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl)piperazine ; SCAM ; substituted cysteine accessibility method ; PNGF ; glycopeptidase-F ; MTSET ; [2-(trimethylammonium)ethyl]-methanethiosulfonate ; M
- 刊名：Neurochemistry International
- 出版年：July 2014
- 年：2014
- 卷：73
- 期：Complete
- 页码：16-26
- 全文大小：2241 K
文摘
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Uptake inhibitor binding induces protease resistance of DAT at residues in EL2.
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These changes may be associated with the mechanism of transport inhibition.
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Modeling of DAT with LeuT indicates a potential salt bridge between D174 and R218.
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These findings suggest a link between EL2 and transport inhibitor action.