摘要
PepT1是一种主要分布于小肠的寡肽转运器,对食物中蛋白质水解所得的二肽和三肽的胃肠道吸收发挥着重要作用。通过化学修饰,使一些膜通透性差的药物对PepT1具有一定的亲和力,能经PepT1转运透过细胞膜,以改善药物的膜通透性,达到提高药物口服生物利用度的目的,这一策略已成为当前口服靶向前药研究领域中的热点。综述近年来PepT1靶向前药的研究进展,包括PepT1的转运机制、PepT1底物的模型以及不同结构类别的该转运器靶向前药实例。
Peptide Transporter 1（PepT1）,which is predominantly distributed throughout the small intestine,plays an important role in the absorption of di-and tripeptides from the digestion of ingested protein.A lot of poorly absorbed drugs have been modified into prodrugs by affinity for PepT1 to improve permeability across intestinal membrane,and eventually to enhance the oral bioavailability of the drugs.Recently,this strategy has become a hot topic of research on targeted prodrug.This review has addressed progress of the prodrugs targeted to PepT1 in recent years,including transport mechanism of PepT1,substrate templet for binding to PepT1,and classic PepT1-targeted prodrugs with different structures.
出处
《药学进展》
CAS
2011年第1期15-22,共8页
Progress in Pharmaceutical Sciences
基金
国家自然科学基金(No.81001413)
教育部新教师基金(No.20090096120002)
国家重大新药创制科技重大专项(No.2009ZX09310-004)
关键词
靶向前药
寡肽转运器1
转运机制
酯类前药
targeted prodrug
Peptide Transporter 1
transport mechanism
ester prodrug
