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Developmental Expression of PEPT1 and PEPT2 in Rat Small Intestine, Colon, and Kidney
The findings suggest that intestinal expression of PEPT1 is induced postpartum, possibly by suckling, and again at the time of weaning, and that the colon may participate in peptide transport early in life. Expand
Cynomolgus Monkey as a Potential Model to Assess Drug Interactions Involving Hepatic Organic Anion Transporting Polypeptides: In Vitro, In Vivo, and In Vitro-to-In Vivo Extrapolation
The cynomolgus monkey has the potential to serve as a useful model for the assessment of OATP-mediated DDIs in a nonclinical setting and a number of in vitro–in vivo extrapolation approaches were explored. Expand
Coproporphyrins in Plasma and Urine Can Be Appropriate Clinical Biomarkers to Recapitulate Drug-Drug Interactions Mediated by Organic Anion Transporting Polypeptide Inhibition
It is concluded that CP-I and CP-III in plasma and urine can be appropriate endogenous biomarkers specifically and reliably reflecting OATP inhibition, and thus the measurement of these molecules can serve as a useful tool to assess OatP drug-drug interaction liabilities in early clinical studies. Expand
Characterization of Organic Anion Transporter 2 (SLC22A7): A Highly Efficient Transporter for Creatinine and Species-Dependent Renal Tubular Expression
The findings revealed the important role of OAT2 in renal secretion and possible reabsorption of creatinine and suggested a molecular basis for potential species difference in the transporter handling of Creatinine. Expand
Localization of PEPT1 and PEPT2 proton-coupled oligopeptide transporter mRNA and protein in rat kidney.
The results conclusively demonstrate that although PEPT1 is expressed in early regions of the proximal tubule (pars convoluta), P EPT2 is specific for the latter regions of proximal Tubule ( pars recta). Expand
Coproporphyrins I and III as Functional Markers of OATP1B Activity: In Vitro and In Vivo Evaluation in Preclinical Species
  • Hong Shen, Jun Dai, +7 authors Y. Lai
  • Biology, Medicine
  • The Journal of Pharmacology and Experimental…
  • 1 May 2016
It is concluded that CPs I and III in plasma and urine are novel endogenous biomarkers reflecting hepatic OATP function, and the measurements have the potential to be incorporated into the design of early clinical evaluation. Expand
Immunolocalization of the proton-coupled oligopeptide transporter PEPT2 in developing rat brain.
The apical expression of PEPT2 in choroid plexus suggests that it is involved in the export of neuropeptides, peptide fragments, and peptide-like drugs from cerebrospinal fluid, especially during early development. Expand
Comparative Evaluation of Plasma Bile Acids, Dehydroepiandrosterone Sulfate, Hexadecanedioate, and Tetradecanedioate with Coproporphyrins I and III as Markers of OATP Inhibition in Healthy Subjects
Investigation of bile acids and fatty acid dicarboxylates in plasma as endogenous probes for OATP inhibition and compared these candidate probes to CPs confirmed that CPs are novel biomarkers suitable for clinical use. Expand
Targeted Disruption of the PEPT2 Gene Markedly Reduces Dipeptide Uptake in Choroid Plexus*
Novel findings provide strong evidence that, under the experimental conditions of this study, PEPT2 is the primary member of the peptide transporter family responsible for dipeptide uptake in choroid plexus tissue. Expand
Role of PEPT2 in peptide/mimetic trafficking at the blood-cerebrospinal fluid barrier: studies in rat choroid plexus epithelial cells in primary culture.
It is demonstrated for the first time that PEPT2 protein is present at the apical membrane of choroidal epithelial cells and that it is functionally active at this membrane surface, suggesting that PepT2 may have a role in the efflux of peptides and/or mimetics from cerebrospinal fluid to the blood. Expand