ArticleBritish journal of pharmacology1994
Substrate specificity of the di/tripeptide transporter in human intestinal epithelia (Caco-2): identification of substrates that undergo H(+)-coupled absorption.
Article in British journal of pharmacology, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 62 citations in OpenAlex.
- Explorative Analysis of Antioxidant, Anti-Inflammatory, and Intestinal Barrier Protective Effects of In Vitro Digested Chickpea- and Dark Chocolate-Based Snack: Insights from Caco-2 and THP-1 Cell Models.Antioxidants (Basel, Switzerland) · 2025Article
- Oligopeptide Transport in Rat Lung Alveolar Epithelial Cells is Mediated by Pept2.Pharmaceutical research · 2017Article
- TEER measurement techniques for in vitro barrier model systems.Journal of laboratory automation · 2015Review
- Reduced colonic microbial diversity is associated with colitis in NHE3-deficient mice.American journal of physiology. Gastrointestinal and liver physiology · 2013Article
- Mutagenesis and cysteine scanning of transmembrane domain 10 of the human dipeptide transporter.Pharmaceutical research · 2009Article
- Quantitative evaluation of PEPT1 contribution to oral absorption of cephalexin in rats.Pharmaceutical research · 2009Article
- Nutrient sensing in the gastrointestinal tract: possible role for nutrient transporters.Journal of physiology and biochemistry · 2008Review
- H+-coupled nutrient, micronutrient and drug transporters in the mammalian small intestine.Experimental physiology · 2007Review
- Demonstration of functional dipeptide transport with expression of PEPT2 in guinea pig cardiomyocytes.Pflugers Archiv : European journal of physiology · 2007Article
- Inhibition of intestinal dipeptide transport by the neuropeptide VIP is an anti-absorptive effect via the VPAC1 receptor in a human enterocyte-like cell line (Caco-2).British journal of pharmacology · 2003Article
- PEPT1-mediated cefixime uptake into human intestinal epithelial cells is increased by Ca2+ channel blockers.Antimicrobial agents and chemotherapy · 2002Article
- H(+)/solute-induced intracellular acidification leads to selective activation of apical Na(+)/H(+) exchange in human intestinal epithelial cells.The Journal of clinical investigation · 1999Article
- Regulation of intracellular pH during H+-coupled oligopeptide absorption in enterocytes from guinea-pig ileum.The Journal of physiology · 1998Article
- Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells.Pharmaceutical research · 1996Article
- Stereoselective uptake of beta-lactam antibiotics by the intestinal peptide transporter.British journal of pharmacology · 1995Article
- D-cycloserine transport in human intestinal epithelial (Caco-2) cells: mediation by a H(+)-coupled amino acid transporter.British journal of pharmacology · 1995Article
- Angiotensin-converting enzyme (ACE) inhibitor transport in human intestinal epithelial (Caco-2) cells.British journal of pharmacology · 1995Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
1. pH-dependent transepithelial transport and intracellular accumulation of the hydrolysis-resistant dipeptide glycylsarcosine (Gly-Sar) have been demonstrated in the model human intestinal epithelial cell line, Caco-2. 2. Experiments with BCECF (2',7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein)-loaded Caco-2 cells demonstrated that dipeptide (Gly-Sar) transport across the apical membrane is coupled to proton flow into the cell. 3. A range of postulated substrates for the intestinal di/tripeptide carrier were tested for their abilities to: (a) inhibit pH-dependent [14C]Gly-Sar apical-to-basal transport and intracellular accumulation and (b) stimulate H+ flow across the apical surface of BCECF-loaded Caco-2 cell monolayers. 4. A range of compounds (including Gly-Gly, Leu-Leu, Gly-Gly-Gly, cefadroxil and cephalexin) caused marked acidification of intracellular pH when perfused at the apical surface of Caco-2 cell monolayers. In contrast leucine and D-Leu-D-Leu failed to induce proton flow. The ability to induce proton-flow across the apical surface by these compounds, in this intestinal epithelium, was directly correlated to the relative inhibitory effects on [14C]-Gly-Sar transport and accumulation. 5. The determination of substrate-induced intracellular pH change in the Caco-2 cell system may provide a useful rapid screen for candidate substrates for absorption via H(+)-coupled transport mechanisms such as the intestinal di/tripeptide carrier in an appropriate physiological context.
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