人寡肽转运体hPepT1及其在前药设计中的应用

孙冬黎 曾苏 蒋惠娣

中国药学杂志 ›› 2011, Vol. 46 ›› Issue (3) : 161-165.

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中国药学杂志 ›› 2011, Vol. 46 ›› Issue (3) : 161-165.
综述

人寡肽转运体hPepT1及其在前药设计中的应用

  • 孙冬黎,曾苏,蒋惠娣*
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摘要

目的 综述人寡肽转运体1(hPepT1的结构特点、功能、在生物体内的分布和调控,及其底物的结构特征。方法 通过对国内外近年来对寡肽转运体研究的调研,归纳总结hPepT1的研究现状。结果 hPepT1除转运饮食中二肽/三肽外,在拟肽类药物的摄取中也起关键的作用,如对β-内酰胺类抗生素及血管紧张素转换酶抑制剂的吸收。hPepT1主要在小肠表达,并受多种因素,如激素,表皮生长因子,饮食,疾病等调控。以hPepT1为靶点,对药物进行结构修饰设计前药,以提高母体药物的口服生物利用度是非常有潜力的策略,目前已有许多成功的例子。由于hPepT1的晶体结构尚没有完全阐明,研究者通过各种体内外模型的转运摄取实验,获得了很多关于hPepT1对底物结构要求的信息。结论 通过文献调研,综述了hPepT1结构特点、功能、在生物体内的分布和调控,尤其是其底物的结构特征,强调其在前药设计中的应用。

关键词

人寡肽转运体 / 底物 / 前药 / 结构 / 调控

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导出引用
孙冬黎 曾苏 蒋惠娣. 人寡肽转运体hPepT1及其在前药设计中的应用[J]. 中国药学杂志, 2011, 46(3): 161-165

参考文献


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