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- W2278836224 abstract "Cytochrome P450s (CYPs), UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs) are the most important enzymes for metabolic clearance. Characterization of phase I and phase II metabolism of a given drug in cellular models is therefore important for an adequate interpretation of the role of drug metabolism in toxicity. We investigated phase I (CYP) and phase II (UGT and SULT) metabolism of three drugs related to drug-induced liver injury (DILI), namely acetaminophen (APAP), diclofenac (DF) and tolcapone (TC), in cryopreserved primary human hepatocytes from 5 donors in suspension and monolayer. The general phase II substrate 7-hydroxycoumarin (7-HC) was included for comparison. Our results show that the decrease in CYP, UGT and SULT activity after plating is substrate dependent. As a consequence the phase I/phase II metabolism ratio is significantly affected, with a shift in monolayer towards phase I metabolism for TC and towards phase II metabolism for APAP and DF. Inter-donor variability in drug metabolism is significant, especially in sulfation of 7-HC or APAP. As CYP, UGT and SULT metabolism may lead to bioactivation and/or detoxification of drugs, a changed ratio in phase I/phase II metabolism may have important consequences for metabolism-related toxicity." @default.
- W2278836224 created "2016-06-24" @default.
- W2278836224 creator A5010946785 @default.
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- W2278836224 date "2016-06-01" @default.
- W2278836224 modified "2023-09-23" @default.
- W2278836224 title "Inter-donor variability of phase I/phase II metabolism of three reference drugs in cryopreserved primary human hepatocytes in suspension and monolayer" @default.
- W2278836224 cites W1416078005 @default.
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- W2278836224 cites W1591613432 @default.
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- W2278836224 cites W1974803439 @default.
- W2278836224 cites W1975903892 @default.
- W2278836224 cites W1978796264 @default.
- W2278836224 cites W1979501124 @default.
- W2278836224 cites W1982311374 @default.
- W2278836224 cites W1982583749 @default.
- W2278836224 cites W1989300686 @default.
- W2278836224 cites W1992475241 @default.
- W2278836224 cites W1993047099 @default.
- W2278836224 cites W1997022318 @default.
- W2278836224 cites W2000585507 @default.
- W2278836224 cites W2001023527 @default.
- W2278836224 cites W2003368011 @default.
- W2278836224 cites W2005101461 @default.
- W2278836224 cites W2010346301 @default.
- W2278836224 cites W2010427019 @default.
- W2278836224 cites W2014869287 @default.
- W2278836224 cites W2016623506 @default.
- W2278836224 cites W2021387395 @default.
- W2278836224 cites W2026833351 @default.
- W2278836224 cites W2033482222 @default.
- W2278836224 cites W2035867345 @default.
- W2278836224 cites W2043169601 @default.
- W2278836224 cites W2047259762 @default.
- W2278836224 cites W2048551332 @default.
- W2278836224 cites W2050954372 @default.
- W2278836224 cites W2052471647 @default.
- W2278836224 cites W2052919116 @default.
- W2278836224 cites W2056361728 @default.
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- W2278836224 cites W2072010935 @default.
- W2278836224 cites W2074828925 @default.
- W2278836224 cites W2075966551 @default.
- W2278836224 cites W2088133994 @default.
- W2278836224 cites W2091433175 @default.
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- W2278836224 cites W2104243204 @default.
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- W2278836224 cites W2128916241 @default.
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- W2278836224 cites W2164206878 @default.
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- W2278836224 doi "https://doi.org/10.1016/j.tiv.2016.02.013" @default.
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