β-和γ-二肽及三肽作为寡肽转运体hPepT1的潜在底物。

Beta- and gamma-di- and tripeptides as potential substrates for the oligopeptide transporter hPepT1.

作者信息

Hubatsch Ina, Arvidsson Per I, Seebach Dieter, Luthman Kristina, Artursson Per

机构信息

Department of Pharmacy, Uppsala University, Box 580, SE-751 23 Uppsala, Sweden.

出版信息

J Med Chem. 2007 Oct 18;50(21):5238-42. doi: 10.1021/jm070148u. Epub 2007 Sep 21.

DOI:10.1021/jm070148u

PMID:17887660

Abstract

The hPepT1-mediated transport properties of a series of 11 synthesized beta- and gamma-peptides have been studied in Caco-2 cells. The results show that several of the compounds interact with the peptide transporter, but only two beta-dipeptides act as substrates and are transported across the cell monolayers. These two are less-efficient substrates than alpha-peptides. Larger derivatives than beta-dipeptides do not act as hPepT1 substrates, but instead, they appear to be substrates for P-glycoprotein efflux.

摘要

在Caco-2细胞中研究了一系列11种合成的β-和γ-肽的hPepT1介导的转运特性。结果表明，其中几种化合物与肽转运体相互作用，但只有两种β-二肽作为底物并跨细胞单层转运。这两种β-二肽作为底物的效率低于α-肽。比β-二肽更大的衍生物不是hPepT1的底物，相反，它们似乎是P-糖蛋白外排的底物。