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Exploring the Metabolism of Loxoprofen in Liver Microsomes: The Role of Cytochrome P450 and UDP-Glucuronosyltransferase in Its Biotransformation
Published 2018-08-01Subjects: Get full text
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282
A frequent CYP2D6 variant promotes skipping of exon 3 and reduces CYP2D6 protein expression in human liver samples
Published 2023-07-01“…Here, using fragment analysis and RT-qPCR, we revealed that rs1058164 G (MAF = 27%–43%) is associated with increased formation of CYP2D6∆E3 in human liver samples (1.4–2.5-fold) and transfected cells. …”
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283
Identification of the Putative Binding Site of a Benzimidazole Opioid (Etazene) and Its Metabolites at µ-Opioid Receptor: A Human Liver Microsomal Assay and Systematic Computational Study
Published 2023-02-01“…In the present study, we investigated the metabolism of etazene in human liver microsomes using ultra-high-performance liquid chromatography–mass spectrometry (UHPLC–MS). …”
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284
Strong and Selective Inhibitory Effects of the Biflavonoid Selamariscina A against CYP2C8 and CYP2C9 Enzyme Activities in Human Liver Microsomes
Published 2020-04-01“…In this study we evaluate the inhibitory potential of five biflavonoids against nine P450 activities (P450s1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A) in human liver microsomes (HLMs) using cocktail incubation and liquid chromatography-tandem mass spectrometry (LC–MS/MS). …”
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285
Identification and cross-species comparison of in vitro phase I brevetoxin (BTX-2) metabolites in northern Gulf of Mexico fish and human liver microsomes by UHPLC-HRMS(/MS)
Published 2023-09-01“…Our results showed that both fish and human liver microsomes rapidly depleted BTX-2, resulting in a 72–99% reduction within 1 h of incubation. …”
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286
A Fast LC-MS/MS Methodology for Estimating Savolitinib in Human Liver Microsomes: Assessment of Metabolic Stability Using In Vitro Metabolic Incubation and In Silico Software Analysis
Published 2023-08-01“…The current work aimed to develop a rapid, specific, green, and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) methodology for estimating savolitinib (SVB) in human liver microsomes (HLMs) with application to an in vitro metabolic stability assessment of SVB in HLMs. …”
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The Propensity of the Human Liver to Form Large Lipid Droplets Is Associated with PNPLA3 Polymorphism, Reduced INSIG1 and NPC1L1 Expression and Increased Fibrogenetic Capacity
Published 2021-06-01“…Hepatocytes with large droplet (Ld-MaS) or small droplet (Sd-MaS) macrovesicular steatosis may coexist in the human liver, but the factors associated with the predominance of one type over the other, including hepatic fibrogenic capacity, are unknown. …”
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Pharmacokinetic Herb-Drug Interactions of Xiang-Sha-Liu-Jun-Zi-Tang and Paclitaxel in Male Sprague Dawley Rats and Its Influence on Enzyme Kinetics in Human Liver Microsomes
Published 2022-04-01“…The influence of XSLJZT on enzyme activity was evaluated using human liver microsomes, and a liquid chromatography-tandem mass spectrometric system was developed to monitor paclitaxel levels in rat plasma. …”
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291
Transcription Factors and ncRNAs Associated with <i>CYP3A</i> Expression in Human Liver and Small Intestine Assessed with Weighted Gene Co-Expression Network Analysis
Published 2022-11-01“…Since long non-coding RNAs (lncRNAs) likely contribute to such networks, we assessed the regulatory effects of both TFs and lncRNAs on <i>CYP3A</i> expression in the human liver and small intestine, main organs of CYP3A expression. …”
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In Vitro Liver Metabolism of Six Flavonoid C-Glycosides
Published 2021-11-01Subjects: Get full text
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294
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<i>Acanthaster planci</i> Inhibits PCSK9 Gene Expression via Peroxisome Proliferator Response Element (PPRE) and Activation of MEK and PKC Signaling Pathways in Human Liver Cells
Published 2022-02-01“…Using real-time PCR, it was shown that the selected <i>A. planci</i> fraction reduced the gene expression of PCSK9 in human liver HepG2 cells. Immunocytochemistry analysis demonstrated that the selected <i>A. planci</i> fraction increased the LDLR protein level and LDL-C uptake in HepG2 cells. …”
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Transcriptome-Wide Analysis of Human Liver Reveals Age-Related Differences in the Expression of Select Functional Gene Clusters and Evidence for a PPP1R10-Governed ‘Aging Cascade’
Published 2021-11-01“…A transcriptome-wide analysis of human liver for demonstrating differences between young and old humans has not yet been performed. …”
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Prospective Prediction of Dapaconazole Clinical Drug–Drug Interactions Using an In Vitro to In Vivo Extrapolation Equation and PBPK Modeling
Published 2022-12-01Subjects: Get full text
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300
LC-HRMS-Based Identification of Transformation Products of the Drug Salinomycin Generated by Electrochemistry and Liver Microsome
Published 2022-01-01Subjects: Get full text
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