Hiroki Kamioka

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The study investigated whether quinolone antibiotics inhibit the PEPT1-mediated uptake of its substrates. Among the quinolones examined, lomefloxacin, moxifloxacin (MFLX) and purlifloxacin significantly inhibited the uptake of PEPT1 substrate phenylalanine-Ψ(CN-S)-alanine (Phe-Ψ-Ala) in HeLa/PEPT1 cells to 31.6 ± 1.3%, 27.6 ± 2.9%, 36.8 ± 2.2% and 32.6 ±(More)
We investigated the influence of sweet and umami (savory) tastants on the intestinal absorption of cephalexin (CEX), a substrate of peptide transporter 1 (PEPT1, SLC15A1) in rats. After oral administration of glucose or mannitol to rats, CEX was administered together with a second dose of glucose or mannitol. Western blot analysis indicated that expression(More)
L-Phenylalanyl-Ψ[CS-N]-l-alanine (Phe-Ψ-Ala), a thiourea dipeptide, was evaluated as a probe for peptide transporter 1 (PEPT1). Uptake of Phe-Ψ-Ala in PEPT1-overexpressing HeLa cells was significantly higher than that in vector-transfected HeLa cells and the Km value was 275 ± 32 µM. The uptake was pH-dependent, being highest at pH 6.0, and was(More)
Drug-induced liver injury (DILI) is a common reason for withdrawal of candidate drugs from clinical trials, or of approved drugs from the market. DILI may be induced not only by intact parental drugs, but also by metabolites or intermediates, and therefore should be evaluated in the enzyme-induced state. Here, we present a protocol for assay of(More)
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