What is PepT1?
PepT1 (also designated SLC15A1) is a proton-coupled peptide transporter expressed on the apical membrane of intestinal epithelial cells. The molecular gateway for KPV cellular uptake in the published intestinal-inflammation research framework.
What the research literature says
PepT1 is a 708-amino-acid integral membrane protein that uses an inward-directed proton gradient to drive uptake of di- and tripeptides from the intestinal lumen into intestinal epithelial cells. The transporter has broad substrate specificity within the di- and tripeptide range; specific peptide substrates are taken up at variable rates depending on sequence and charge.
KPV’s research framework centres on PepT1-mediated uptake at the intestinal mucosa. The Dalmasso PepT1-uptake characterisation paper established that the tripeptide KPV is taken up via PepT1 and that the uptake step concentrates the compound at the site of action (PMID 18061177). The Viennois colitis-associated cancer work documented critical PepT1 involvement (PMID 27458604). The Xiao orally-targeted-delivery work used hyaluronic-acid-functionalised nanoparticles as a strategy to maximise PepT1-mediated uptake (PMID 28143741).
PepT1 expression is upregulated in inflamed intestinal tissue, which contributes to KPV’s selective accumulation at the site of action in IBD-research models — the inflammation that the compound is studied to attenuate also drives the uptake mechanism that delivers the compound to the affected tissue.
Why this matters in research context
PepT1 matters in peptide-research contexts almost entirely as the molecular gateway for KPV’s intestinal-mucosa pharmacology. Researchers using KPV outside the intestinal-inflammation framework may see different (and less characterised) pharmacology because the PepT1-uptake pathway is less operative in non-intestinal tissues.
Related compounds
- KPV 10mg — PepT1-substrate research
Related research questions
References
- Dalmasso G et al. PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. Gastroenterology 2008;134(1):166-178. [PMID 18061177]
- Viennois E et al. Critical role of PepT1 in promoting colitis-associated cancer and therapeutic benefits of the anti-inflammatory PepT1-mediated tripeptide KPV in a murine model. Cell Mol Gastroenterol Hepatol 2016;2(3):340-357. [PMID 27458604]
- Xiao B et al. Orally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative Colitis. Mol Ther 2017;25(7):1628-1640. [PMID 28143741]
Research-questions pages describe research-context use of peptide-research terminology. They do not constitute medical, veterinary, or clinical advice. Every compound in the Ronin catalog is sold strictly for laboratory and research use only.