文章基本信息

标题：A single serine residue controls the cation dependence of substrate transport by the rat serotonin transporter
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作者：Cyrille Sur ; Heinrich Betz ; Patrick Schloss 等
期刊名称：Proceedings of the National Academy of Sciences
印刷版ISSN：0027-8424
电子版ISSN：1091-6490
出版年度：1997
卷号：94
期号：14
页码：7639-7644
DOI：10.1073/pnas.94.14.7639
语种：English
出版社：The National Academy of Sciences of the United States of America
摘要：The serotonin transporter (SERT) is a member of the Na+/Cl--dependent neurotransmitter transporter family and constitutes the target of several clinically important antidepressants. Here, replacement of serine-545 in the recombinant rat SERT by alanine was found to alter the cation dependence of serotonin uptake. Substrate transport was now driven as efficiently by LiCl as by NaCl without significant changes in serotonin affinity. Binding of the antidepressant [3H]imipramine occurred with 1/5th the affinity, whereas [3H]citalopram binding was unchanged. These results indicate that serine-545 is a crucial determinant of both the cation dependence of serotonin transport by SERT and the imipramine binding properties of SERT.
关键词：neurotransmitter ; uptake ; antidepressant binding ; mutagenesis