Mammalian peptide transporters as targets for drug delivery

Isabel Rubio-Aliaga, Hannelore Daniel

Research output: Contribution to journalReview articlepeer-review

244 Scopus citations


Peptide transporters are integral plasma membrane proteins that mediate the cellular uptake of dipeptides and tripeptides in addition to a variety of peptidomimetics. The carriers, which occur predominantly in the brush-border membranes of epithelial cells of the small intestine, lung, choroid plexus and kidney, contribute to absorption, distribution and elimination of their substrates. The cellular uptake of peptides and peptidomimetics involves the cotransport of protons down an inwardly directed, electrochemical proton gradient that provides the driving force and causes the electrogenicity of the translocation step. Peptide transporters represent excellent targets for the delivery of pharmacologically active compounds because their substrate-binding site can accommodate a wide range of molecules of differing size, hydrophobicity and charge.

Original languageEnglish
Pages (from-to)434-440
Number of pages7
JournalTrends in Pharmacological Sciences
Issue number9
StatePublished - 1 Sep 2002


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