Human variability in isoform-specific UDP-glucuronosyltransferases: markers of acute and chronic exposure, polymorphisms and uncertainty factors
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DOI: 10.1007/s00204-020-02765-8
Abstract: UDP-glucuronosyltransferases (UGTs) are involved in phase II conjugation reactions of xenobiotics and differences in their isoform activities result in interindividual kinetic differences of UGT probe substrates. Here, extensive literature searches were performed to identify probe… read more here.
Keywords: uncertainty; uncertainty factors; isoform; probe substrates ... See more keywords
Molecular probes for human cytochrome P450 enzymes: Recent progress and future perspectives
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DOI: 10.1016/j.ccr.2020.213600
Abstract: Abstract The cytochrome P450 enzymes (P450s or CYPs) are a class of heme-containing monooxygenases responsible for the oxidative metabolism of a wide range of endogenous substances and foreign chemicals. Deciphering the physiological functions of CYPs… read more here.
Keywords: cytochrome p450; probes human; p450 enzymes; probe substrates ... See more keywords
Substrate and method dependent inhibition of three ABC‐transporters (MDR1, BCRP, and MRP2)
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DOI: 10.1016/j.ejps.2017.03.002
Abstract: ABSTRACT Drug transport and drug‐drug interactions (DDI) with human ABC transporters are generally investigated in mammalian cell lines or inverted membrane vesicles from insect cells (Sf9) overexpressing the transporter of interest. In this study, we… read more here.
Keywords: abc transporters; mrp2; inhibition; probe substrates ... See more keywords
Pharmacokinetic drug interactions of asciminib with the sensitive cytochrome P450 probe substrates midazolam, warfarin, and repaglinide in healthy participants
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DOI: 10.1111/cts.13252
Abstract: Asciminib, a first‐in‐class BCR‐ABL1 inhibitor that works by Specifically Targeting the ABL Myristoyl Pocket (STAMP), is a new treatment option for patients with chronic myeloid leukemia who no longer benefit from currently approved tyrosine kinase… read more here.
Keywords: healthy participants; warfarin repaglinide; probe substrates; cytochrome p450 ... See more keywords