【摘要】 小肠上皮细胞刷状缘侧的寡肽转运蛋白(PEPT1)以及侧底膜的寡肽转运蛋白是寡肽转运蛋白(PEPT)的2种亚型,它们在寡肽及拟肽类药物(peptidomimetic drug)肠转运中发挥重要作用。通过前体药物(prodrug)设计将一些吸收差的药物修饰成类似二肽或三肽的结构,在PEPT1的介导下吸收,能够提高这些药物的口服生物利用度,这是非常有意义的。更多还原

【Abstract】 Peptide transporters that expressed in the intestinal brush border membrane (PEPT1) and peptide transporter that expressed in the basolateral membrane were the two subtypes of peptide transporter (PEPT) . They played an essential role in absorption of oligopeptides and peptidomimetic drugs. PEPT1 was a key target for approach of prodrug. Not well absorbed drugs could be appropriately designed in the form of di-/ tripeptide analogues to be well absorbed across the intestinal brush border membrane via PEPT1 and thus increase the valuable oral bioavailability.更多还原