Quantitative targeted absolute proteomics for 28 human transporters in plasma membrane of Caco-2 cell monolayer cultured for 2, 3, and 4 weeks

Drug Metabolism and Pharmacokinetics
Yasuo UchidaTetsuya Terasaki

Abstract

The purpose of the present study was to evaluate and compare the absolute protein expression levels of 28 drug-related transporters in Caco-2 cell monolayers cultured for 2, 3, and 4 weeks. Plasma membrane fractions of Caco-2 cells cultured on Transwell inserts for 2, 3 and 4 weeks were prepared and digested with trypsin, and then simultaneous absolute quantification of 28 transporters and Na(+)/K(+)-ATPase was conducted using our established quantitative targeted absolute proteomic technique. Nine transporters and Na(+)/K(+)-ATPase were detected. MDR1, BCRP, PEPT1, OSTα and OSTβ were highly expressed (greater than 1 fmol/μg protein), while MRP2, MRP4, OATP2B1 and MCT1 were moderately expressed (0.328-0.871 fmol/μg protein). No significant difference was observed in the protein expression levels of these transporters or Na(+)/K(+)-ATPase among the 2-, 3- and 4-week cultures. The other 19 transporters, including MRP1, MRP3, OATP1A2, OATP3A1, OATP4A1, and OATP1B3, were not detected. This information about the rank order of transporter protein expression will be useful to predict what transporter(s) are likely or unlikely to influence the permeability of various compounds across monolayers of Caco-2 cells, which are widely used in...Continue Reading

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Citations

Feb 13, 2016·Journal of Pharmaceutical Sciences·Magnus ÖlanderPer Artursson
Mar 10, 2016·Journal of Pharmaceutical Sciences·Matthew D HarwoodGeoffrey Warhurst
Sep 10, 2015·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Agnieszka Anna Rawłuszko-WieczorekPaweł Piotr Jagodziński
Feb 13, 2016·Journal of Pharmaceutical Sciences·Ivailo SimoffPer Artursson
Dec 13, 2016·Journal of Pharmaceutical Sciences·Bhagwat PrasadDeepak Kumar Bhatt
Apr 27, 2016·Molecular Pharmacology·Zainab M MahdiBruno Stieger
Jul 28, 2020·Cellular and Molecular Life Sciences : CMLS·Anna MeyfourGhasem Hosseini Salekdeh
Feb 9, 2017·Stem Cells Translational Medicine·Kenneth R Boheler, Rebekah L Gundry
Jul 16, 2019·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Yulin WangThomas Efferth
Apr 2, 2021·Biological & Pharmaceutical Bulletin·Yasuo Uchida
Jan 17, 2020·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·E JacquerouxX Delavenne
May 4, 2021·Frontiers in Pharmacology·Christoph WenzelStefan Oswald
May 7, 2021·Biological & Pharmaceutical Bulletin·Kaori MorimotoMikio Tomita

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