论文部分内容阅读
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。
PepT1 is an oligopeptide transporter mainly distributed in the small intestine and plays an important role in the gastrointestinal absorption of dipeptides and tripeptides obtained from the hydrolysis of proteins in foods. Through chemical modification, some drugs with poor membrane permeability have certain affinity to PepT1 and can be transported through the cell membrane via PepT1 to improve the membrane permeability of the drug, so as to improve the oral bioavailability of the drug. This strategy has been adopted Has become a hot spot in the field of orally-targeted prodrugs. In this paper, we review the research progress of PepT1 targeting prodrugs in recent years, including the transport mechanism of PepT1, the model of PepT1 substrate and some examples of this transporter targeting prodrugs of different structural classes.