Abstract
This review is an update of the review published in this journal in 2002. Over the past two years a number of studies have investigated peptide transporter (mainly hPEPT1) substrate binding. Cysteine scanning mutagenesis has revealed important information about structural aspects of the PEPT1 pro-tein. Pharmaceutical formulation strategies have been investigated in order to increase oral absorption of PEPT1 substrates by maintaining controlled pH conditions. New research disciplines, such as pharmacogenomics/genetics, have also had an impact on the field. Variations in the genes SLC15A1 and SLC15A2, coding for hPEPT1 and hPEPT2, respectively, have been investigated. The recent advances within the understanding of PEPT1 substrate pharmacophore properties, PEPT1 structure and population genet-ics, are reviewed and their possible significance in drug design, drug delivery and pharmacokinetics are discussed.