Bioluminescence Measurement of Time-Dependent Dynamic Changes of CYP-Mediated Cytotoxicity in CYP-Expressing Luminescent HepG2 Cells

CYP-Mediated Sulfoximine Deimination of AZD6738.

In hepatic S9 and human liver microsomes (HLMs) the sulfoximine moiety of the ATR inhibitor AZD6738 is metabolized to its corresponding sulfoxide (AZ8982) and sulfone (AZ0002). The initial deimination to AZ8982 is nominally a reductive reaction, but in HLMs it required both NADPH and oxygen and also was inhibited by 1-aminobenzotriazole at a concentration of 1 mM. Studies conducted in a panel o...

Zebularine upregulates expression of CYP genes through inhibition of DNMT1 and PKR in HepG2 cells

Drug-induced hepatotoxicity is one of the major reasons cited for drug withdrawal. Therefore, it is of extreme importance to detect human hepatotoxic candidates as early as possible during the drug development process. In this study, we aimed to enhance hepatocyte functions such as CYP gene expression in HepG2 cells, one of the most extensively used cell lines in evaluating hepatotoxicity of ch...

Cytochrome P450 (CYP) dependent metabolism in HepaRG cells cultured in a dynamic three-dimensional (3D) bioreactor

DLPC attenuates alcohol-induced cytotoxicity in HepG2 cells expressing CYP2E1.

AIMS Alcoholic liver injury was shown to result largely from oxidative stress generated by ethanol metabolism via cytochrome P4502E1 (CYP2E1). Our aim was to determine whether this could be overcome by using dilinoleoylphosphatidylcholine (DLPC), an innocuous antioxidant extracted from soybeans. METHODS To address this question, we determined whether DLPC protects against alcohol-induced cyto...

Expression and Functional Analysis of CYP 2 D 6 . 24 , CYP 2 D 6 . 26 , CYP 2 D 6 . 27 and CYP 2 D 7

The objectives of this study were to compare the drug-metabolizing activity of human CYP2D6.24 (I297L), CYP2D6.26 (I369T), CYP2D6.27 (E410K) allelic isoforms with wild-type CYP2D6.1, and to express the CYP2D7 protein derived from an indel polymorphism (CYP2D7 138delT) and investigate its possible codeine O-demethylase activity. Successful creation of individual cDNAs corresponding to CYP2D6*24 ...