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Solute carrier family 15 member 2 (PEPT2)
- Target
- PEPT2
- Molecular classification
- Transporter, Proton-coupled oligopeptide transporter, Member of the solute carrier (SLC) family, Multi-pass membrane protein
01
Overview
Solute carrier family 15 member 2 (PEPT2) is a multi-pass membrane transporter expressed predominantly in the kidney, choroid plexus, brain, and other epithelial tissues. PEPT2 mediates the proton-dependent uptake of di- and tripeptides as well as various peptide-like pharmaceuticals and xenobiotics. This transporter plays an essential role in renal reabsorption of small peptides, central nervous system clearance, and is involved in innate immune responses against bacteria. Pharmacogenetic variability in SLC15A2 may significantly impact drug disposition and toxicity, making PEPT2 a notable therapeutic target in drug development and safety pharmacology.
- Other names
- PEPT2Peptide transporter 2Kidney H(+)/peptide cotransporterOligopeptide transporter 2Oligopeptide transporter, kidney isoform
02
Mechanism of action
Drug import/export via proton-coupled transport (2:1 or 3:1 proton to peptide ratio) Influences renal reabsorption, central nervous system clearance, and tissue distribution of peptide-like drugs
03
Biological functions
Dipeptide and tripeptide transmembrane transportProton-coupled cotransportReabsorption of peptides in kidneyClearance of peptidomimetics (peptide-like drugs)Xenobiotic detoxification and transportRegulation of innate immune response via bacterial peptidoglycan uptake
04
Disease associations
Drug pharmacokinetics (influences uptake, efflux, elimination of peptide-like drugs)Lead toxicity (certain SLC15A2 haplotypes associated with higher blood lead burden in children)Possible involvement in infection and innate immunity, as it mediates peptidoglycan transport relevant to NOD-like receptor signaling
05
Safety considerations
Polymorphisms can alter drug absorption and elimination, impacting efficacy/safety of drugs cleared by PEPT2Variation may influence susceptibility to lead toxicity or adverse drug reactions
06
Interacting drugs
Beta-lactam antibiotics (e.g., cefadroxil)
3 more in the full profile.
07
Biomarkers
SLC15A2 genetic variants (e.g., hPEPT2*1, hPEPT2*2 alleles) impact drug response and toxicity; could serve as biomarkers for pharmacogenomics and lead exposure risk
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