SLC15A1 (solute carrier family 15 (oligopeptide transporter), member 1 or PEPT1) encodes a high-capacity, low-affinity proton-coupled oligopeptide transporter expressed in all regions of the small intestine and specifically at the apical side of enterocytes. SLC15A1 also has low, but measurable expression in the proximal and distal segments of the colon. SLC15A1 is involved in the uptake of di/tripeptides , ACE inhibitors, &beta;-lactam antibiotics and other prodrugs (valacyclovir, zanamivir, etc) from the intestinal lumen. Prodrugs are converted from inactive to pharmacologically active drugs when metabolized. In this case, the relevant prodrugs contain an added chemical promoiety that confers Pept1-mediated transport upon the entire molecule allowing for enhanced intestinal absorption. huPEPT1 mice express human SLC15A1 (or PEPT1) on a mouse Slc15a1 deficient background. Mice homozygous for the knock-out allele and hemizygous for the transgene are viable and fertile with no obvious phenotype. These mice may be used as a humanized mouse model for studying prodrug absorption and disposition.

huPEPT1 mice express human SLC15A1 (or PEPT1) on a mouse Slc15a1 deficient background. SLC15A1 functions as an intestinal peptide transporter. These mice may be used as a humanized mouse model for studying prodrug absorption and disposition.

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