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Characterization of a Novel CYP1A2 Knockout Rat Model Constructed by CRISPR/Cas9(S)

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (8)

CYP1A2, as one of the most important cytochrome P450 isoforms, is involved in the biotransformation of many important endogenous and exogenous substan......

Silybin Restored CYP3A Expression through the Sirtuin 2/Nuclear Factor kappa-B Pathway in Mouse Nonalcoholic Fatty Liver Disease

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (9)

Silybin is widely used as a hepatoprotective agent in various liver disease therapies and has been previously identified as a CYP3A inhibitor. However......

Differences in Hydrolase Activities in the Liver and Small Intestine between Marmosets and Humans

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (9)

For drug development, species differences in drug-metabolism reactions present obstacles for predicting pharmacokinetics in humans. We characterized t......

Tertiary Oxidation of Deoxycholate Is Predictive of CYP3A Activity in Dogs

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (5)

Deoxycholic acid (DCA, 3 alpha, 12 alpha-dihydroxy-5 beta-cholan-24-oic acid) is the major circulating secondary bile acid, which is synthesized by gu......

Metabolic Retroversion of Piperaquine (PQ) via Hepatic Cytochrome P450-Mediated N-Oxidation and Reduction: Not an Important Contributor to the Prolonged Elimination of PQ

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (5)

As a partner antimalarial with an extremely long elimination half-life (similar to 30 days), piperaquine (PQ) is mainly metabolized into a pharmacolog......

Reversible and Irreversible Inhibition of Cytochrome P450 Enzymes by Methylophiopogonanone A

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (6)

Methylophiopogonanone A (MOA), an abundant homoisoflavonoid bearing a methylenedioxyphenyl moiety, is one of the major constituents in the Chinese her......

Identification of Triterpene Acids in Poria cocos Extract as Bile Acid Uptake Transporter Inhibitors

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (5)

Literature reports that Poria cocos reduces blood lipid levels; however, the underlying mechanism remains unclear. Blood lipid levels are closely rela......

Functional Proliferating Human Hepatocytes: In Vitro Hepatocyte Model for Drug Metabolism, Excretion, and Toxicity

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (4)

To develop a functional alternative hepatocyte model for primary human hepatocytes (PHHs) with proliferative property, essential drug metabolic, and t......

The Long Noncoding RNA Hepatocyte Nuclear Factor 4a Antisense RNA 1 Negatively Regulates Cytochrome P450 Enzymes in Huh7 Cells via Histone Modifications

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (5)

Y The maintenance of homeostasis of cytochromes P450 enzymes (P450s) under both physiologic and xenobiotic exposure conditions is ensured by the actio......

Sex-, Age-, and Race/Ethnicity-Dependent Variations in Drug-Processing and NRF2-Regulated Genes in Human Livers

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (1)

Individual variations in xenobiotic metabolism affect the sensitivity to diseases. In this study, the impacts of sex, age, and race/ethnicity on drug-......

Effect of Gender and Various Diets on Bile Acid Profile and Related Genes in Mice

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (1)

Diet is an important factor for many diseases. Previous studies have demonstrated that several diets had remarkable effects on bile acid (BA) homeosta......

Prediction of Transporter-Mediated Rosuvastatin Hepatic Uptake Clearance and Drug Interaction in Humans Using Proteomics-Informed REF Approach

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (2)

Suspended, plated, or sandwich-cultured human hepatocytes are routinely used for in vitro to in vivo extrapolation (IVIVE) of transporter-mediated hep......

The Hypoglycemic Effect of Berberine and Berberrubine Involves Modulation of Intestinal Farnesoid X Receptor Signaling Pathway and Inhibition of Hepatic Gluconeogenesis

期刊: DRUG METABOLISM AND DISPOSITION, 2021; 49 (3)

Our previous study suggests that berberine (BBR) lowers lipids by modulating bile acids and activating intestinal farnesoid X receptor (FXR). However,......

Circadian Clock Component Rev-erb alpha Regulates Diurnal Rhythm of UDP-Glucuronosyltransferase 1a9 and Drug Glucuronidation in Mice

期刊: DRUG METABOLISM AND DISPOSITION, 2020; 48 (8)

UDP-glucuronosyltransferases (UGTs) are a family of phase II enzymes that play an important role in metabolism and elimination of numerous endo- and x......

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