Issue 5, 2016

A cyclosporine derivative is a substrate of the oligopeptide transporter PepT1

Abstract

The mammalian proton-coupled oligopeptide transporter PepT1 is recognised as an important route of oral drug delivery. Peptide-based compounds offer great potential as drugs but their application is limited by poor membrane permeability, amongst other challenges. Using cyclosporin A as a proof-of-concept, we demonstrate for the first time that peptidic molecules over 1000 Da in size can be targeted towards and transported by PepT1.

Graphical abstract: A cyclosporine derivative is a substrate of the oligopeptide transporter PepT1

Article information

Article type
Research Article
Submitted
12 Dec 2015
Accepted
12 Mar 2016
First published
15 Mar 2016

Med. Chem. Commun., 2016,7, 999-1002

A cyclosporine derivative is a substrate of the oligopeptide transporter PepT1

D. W. Foley, I. Bermudez, P. D. Bailey and D. Meredith, Med. Chem. Commun., 2016, 7, 999 DOI: 10.1039/C5MD00575B

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