Solute carrier family 15 member 1 (SLC15A1)

Solute carrier family 15 member 1 (SLC15A1), commonly known as Peptide transporter 1 (PEPT1), is a proton-coupled oligopeptide transporter primarily localized to the apical membrane of enterocytes in the small intestine. It mediates the uptake of di- and tripeptides, a critical step in dietary protein assimilation, by coupling peptide influx with a proton gradient across the membrane. SLC15A1 also enables the absorption of numerous peptidomimetic drugs, including many β-lactam antibiotics, ACE inhibitors, and antiviral prodrugs, making it highly relevant in pharmacology and drug development. It plays a similar, albeit less prominent, role in renal peptide reabsorption. Alterations in its expression or function can influence disease risk (such as inflammatory bowel disease) and affect the pharmacokinetics of orally administered drugs, positioning SLC15A1 as both a key biological transporter and a significant therapeutic target[1][2][3][5].

Other names

Peptide transporter 1PEPT1Intestinal H+/peptide cotransporterOligopeptide transporter 1HPEPT1HPECT1Caco-2 oligopeptide transporterbA551M18.1.1Small intestine isoformMacrophage oligopeptide transporter PEPT1

Proton-coupled symport, transporting di- and tripeptides (and structurally related drugs) into cells by utilizing the inward electrochemical proton gradient Increases oral bioavailability of peptidomimetic drugs by enabling intestinal uptake