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.