ArticleThe Biochemical journal1994
Expression and protein kinase C-dependent regulation of peptide/H+ co-transport system in the Caco-2 human colon carcinoma cell line.
Article in The Biochemical journal, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 141 citations in OpenAlex.
- Dietary cholesterol increases body levels of oral administered vitamin DJournal of nutritional science · 2024Article
- Molecular Insights to the Structure-Interaction Relationships of Human Proton-Coupled Oligopeptide Transporters (PepTs).Pharmaceutics · 2023Review
- Calcium-sensing receptor regulates intestinal dipeptide absorption via CaPhysiological reports · 2020Article
- Functional characterization of oligopeptide transporter 1 of dairy cows.Journal of animal science and biotechnology · 2018Article
- Protein Kinases C-Mediated Regulations of Drug Transporter Activity, Localization and Expression.International journal of molecular sciences · 2017Review
- Critical role of PepT1 in promoting colitis-associated cancer and therapeutic benefits of the anti-inflammatory PepT1-mediated tripeptide KPV in a murine model.Cellular and molecular gastroenterology and hepatology · 2016Article
- The role and pathophysiological relevance of membrane transporter PepT1 in intestinal inflammation and inflammatory bowel disease.American journal of physiology. Gastrointestinal and liver physiology · 2012Review
- Differentiating passive from transporter-mediated uptake by PepT1: a comparison and evaluation of four methods.The Journal of surgical research · 2011Article
- Crystal structure of a prokaryotic homologue of the mammalian oligopeptide-proton symporters, PepT1 and PepT2.The EMBO journal · 2011Article
- Effect of Different Metal Ions on the Biological Properties of Cefadroxil.Pharmaceuticals (Basel, Switzerland) · 2009Article
- An energy supply network of nutrient absorption coordinated by calcium and T1R taste receptors in rat small intestine.The Journal of physiology · 2009Article
- Ethanol inhibits functional activity of the human intestinal dipeptide transporter hPepT1 expressed in Xenopus oocytes.Alcoholism, clinical and experimental research · 2008Article
- PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation.Gastroenterology · 2008Article
- Stable transfection of MDCK cells with epitope-tagged human PepT1.Pharmaceutical research · 2004Article
- PEPT1-mediated cefixime uptake into human intestinal epithelial cells is increased by Ca2+ channel blockers.Antimicrobial agents and chemotherapy · 2002Article
- PepT1-mediated epithelial transport of dipeptides and cephalexin is enhanced by luminal leptin in the small intestine.The Journal of clinical investigation · 2001Article
- Evidence for overlapping substrate specificity between large neutral amino acid (LNAA) and dipeptide (hPEPT1) transporters for PD 158473, an NMDA antagonist.Pharmaceutical research · 1999Article
- Intestinal transport of beta-lactam antibiotics: analysis of the affinity at the H+/peptide symporter (PEPT1), the uptake into Caco-2 cell monolayers and the transepithelial flux.Pharmaceutical research · 1999Article
- Substrate upregulation of the human small intestinal peptide transporter, hPepT1.The Journal of physiology · 1998Article
- Antisense expression of the peptide transport gene AtPTR2-B delays flowering and arrests seed development in transgenic Arabidopsis plants.Plant physiology · 1997Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The characteristics of the transport of the dipeptide glycylsarcosine were studied in the human colon carcinoma cell line Caco-2 grown as a monolayer on impermeable plastic support. Transport of glycylsarcosine in these cells was found to be Na(+)-independent, but was stimulated by an inwardly directed H+ gradient. This H(+)-dependent transport of glycylsarcosine was inhibited by di- and tri-peptides and also by the beta-lactam antibiotic cephalexin, but was unaffected by the amino acids glycine and leucine. The transport system exhibited a Michaelis-Menten constant (Kt) of 1.1 +/- 0.1 mM for glycylsarcosine. The specific activity of the transport system in this cell line was found to be maximal when the cultures were confluent. Treatment of the cells with phorbol esters which activate protein kinase C resulted in a significant inhibition of the transport system. This inhibition was specific and could be blocked if treatment was done in the presence of staurosporine, an inhibitor of protein kinase C. Kinetic analysis revealed that the inhibition was associated with a decrease in the maximal velocity, the Kt remaining unaffected. The phorbol-ester-induced inhibition of the peptide-transport system was not prevented by co-treatment with cycloheximide, an inhibitor of cellular protein synthesis. In addition, there was no change in the intracellular pH following treatment with the phorbol ester, suggesting that the effect was not due to alterations in the transmembrane pH gradient. It is concluded that the peptide/H+ co-transport system, which is known to exist in the normal intestine, is expressed in Caco-2 cells and that the function of the transport system is under the regulatory control of protein kinase C.
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