寡肽转运载体PepT1广泛分布于人和动物体内的多种器官和组织,其底物主要为蛋白水解后的二肽和三肽。本文综合文献,阐述PepT1的体内分布及其质子依赖型的转运机制,从空间结构的角度分析其对底物分子的选择性,介绍评价底物与PepT1二者问亲和活性的体内外模型及PepT1底物修饰策略在促进药物吸收方面的应用。
Oligopeptide transporter PepT1 is widely distributed in various organs and tissues of human and animals, which substrates are mainly proteolytic dipeptides and tripeptides. Based on a literature review, the in vivo distribution of PeoT1 and its oroton-deoendent transport mechanism are introduced and the structure of the transporter and its selectivity on the substrate molecules are elucidated in this paper. In addition, several in vitro and in vivo models for evaluation of PepTl-mediated transportation as well as the applications of suvstrate modification strategies to drug absorption are also described.