Target intelligence / Profile preview

Proton-coupled oligopeptide transporter 1 (PepT1) or Proton-coupled oligopeptide transporter 2 (PepT2) (PepT1 (SLC15A1), PepT2 (SLC15A2))

Target
PepT1 (SLC15A1), PepT2 (SLC15A2)
Molecular classification
Transporter, Solute Carrier (SLC), Major Facilitator Superfamily (MFS), Proton-coupled transporter
01

Overview

The dipeptide transporter, especially PepT1 and PepT2, are integral membrane proteins belonging to the proton-coupled oligopeptide transporter (POT) family (SLC15A subfamily), responsible for actively transporting di- and tripeptides from the intestinal lumen or renal filtrate into epithelial cells using the proton electrochemical gradient. They play a vital physiological role in protein nutrition and are notable for facilitating the uptake of a variety of clinically relevant drugs. Their structure features 12 transmembrane domains and several key residues critical for substrate and inhibitor binding. Transport is sensitive to inhibition by modified dipeptides, and conformational changes in the transporter govern substrate specificity and kinetics. Drugs targeting PepT1/2 may act as substrates or inhibitors, impacting their therapeutic efficacy and safety profile. If you require a more specific name or context (e.g., human vs. bacterial transporter), please specify, as "dipeptide transporter" can also refer to prokaryotic transporters like DtpA (E. coli), DppD (Bacillus) or others. However, in human and mammalian physiology, "dipeptide transporter" most commonly refers to PepT1 and PepT2.

Other names
Dipeptide transporterPeptide transporter 1 (PepT1)Peptide transporter 2 (PepT2)SLC15A1SLC15A2Proton-coupled oligopeptide transporterPOT family transporter
02

Mechanism of action

Drugs are transported via proton-coupled co-transport, leveraging the proton gradient across epithelia. Competitive inhibition (e.g., some modified dipeptides act as inhibitors)

03

Biological functions

Nutrient absorption (di- and tripeptides)Drug uptake (e.g., penicillins, cephalosporins)Proton-dependent peptide translocation
04

Disease associations

Cancer (upregulated in some tumors)Infection (affects antibiotic bioavailability)Other (affects nutrition, drug metabolism)
05

Safety considerations

Potential for drug-drug interactions due to competition for transportAltered drug bioavailability in disease states or genetic polymorphismsRisk of off-target drug uptake leading to toxicity in tissues with high transporter expression
06

Interacting drugs

Penicillins

6 more in the full profile.

07

Biomarkers

Expression levels of PepT1/PepT2 in tissue as predictors of drug absorptionOral bioavailability of peptide-like drugs

Beyond the preview

Go deeper on Proton-coupled oligopeptide transporter 1 (PepT1) or Proton-coupled oligopeptide transporter 2 (PepT2) (PepT1 (SLC15A1), PepT2 (SLC15A2)).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Proton-coupled oligopeptide transporter 1 (PepT1) or Proton-coupled oligopeptide transporter 2 (PepT2) (PepT1 (SLC15A1), PepT2 (SLC15A2)).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call