ArticlePharmaceutical research2012
Influence of fed-fasted state on intestinal PEPT1 expression and in vivo pharmacokinetics of glycylsarcosine in wild-type and Pept1 knockout mice.
Article in Pharmaceutical research, 2012. 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, 37 citations in OpenAlex.
- Molecular Insights to the Structure-Interaction Relationships of Human Proton-Coupled Oligopeptide Transporters (PepTs).Pharmaceutics · 2023Review
- Quercetin Alleviates Inflammation and Energy Deficiency Induced by Lipopolysaccharide in Chicken Embryos.Animals : an open access journal from MDPI · 2023Article
- Function, Regulation, and Pathophysiological Relevance of the POT Superfamily, Specifically PepT1 in Inflammatory Bowel Disease.Comprehensive Physiology · 2018Review
- Effect of heat stress on protein utilization and nutrient transporters in meat-type chickens.International journal of biometeorology · 2017Article
- Di- and tripeptide transport in vertebrates: the contribution of teleost fish models.Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology · 2017Review
- Expression and regulation of the neutral amino acid transporter B0AT1 in rat small intestine.PloS one · 2017Article
- 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
- Species differences in the pharmacokinetics of cefadroxil as determined in wildtype and humanized PepT1 mice.Biochemical pharmacology · 2016Article
- Transcriptional and functional regulation of the intestinal peptide transporter PEPT1.The Journal of physiology · 2014Review
- Cross-species comparison of genes related to nutrient sensing mechanisms expressed along the intestine.PloS one · 2014Article
- Glucose-dependent insulinotropic polypeptide regulates dipeptide absorption in mouse jejunum.American journal of physiology. Gastrointestinal and liver physiology · 2013Article
- In vivo absorption and disposition of cefadroxil after escalating oral doses in wild-type and PepT1 knockout mice.Pharmaceutical research · 2013Article
- Gene expression of carnosine-related enzymes and transporters in skeletal muscle.European journal of applied physiology · 2013Article
- Relevance of PepT1 in the intestinal permeability and oral absorption of cefadroxil.Pharmaceutical research · 2013Article
- Significance of peptide transporter 1 in the intestinal permeability of valacyclovir in wild-type and PepT1 knockout mice.Drug metabolism and disposition: the biological fate of chemicals · 2013Article
- Proton-coupled oligopeptide transporter family SLC15: physiological, pharmacological and pathological implications.Molecular aspects of medicineReview
- Chemically modified peptides and proteins - critical considerations for oral delivery.Tissue barriersReview
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
purposeTo determine if fasting would affect the intestinal expression and in vivo functional activity of PEPT1 as determined after oral dosing of the dipeptide glycylsarcosine (GlySar).
methodsSystemic exposure and tissue distribution studies were performed in wild-type and Pept1 knockout mice, under fed and fasted conditions, following both intravenous and oral doses of [(14)C]GlySar at 5 nmol/g body weight. Intestinal PEPT1 expression was evaluated by real-time PCR and immunoblot analyses.
resultsWe found that expression of PEPT1 protein in the small intestine was increased ~2-fold in wild-type mice during fasted as compared to fed conditions. In agreement, systemic exposure and peak plasma concentrations of orally administered GlySar were 40 and 65% greater, respectively, in wild-type mice during fasted vs. fed state. No significant differences were observed between fed and fasted animals during PEPT1 ablation. Tissue distribution of GlySar was unchanged after oral dosing for all four treatment groups.
conclusionsAs little as 16 h of fasting can cause significant upregulation of PEPT1 protein expression in the small intestine, which then translates into a significant increase in in vivo oral absorption of GlySar.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.