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An improved staining procedure for the detection of the peroxidase activity of cytochrome P-450 on sodium dodecyl sulfate polyacrylamide gels.
Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cdna-expressed human cytochrome P450.
- A. Ghosal, H. Satoh, P. Thomas, E. Bush, D. Moore
- Biology, ChemistryDrug Metabolism And Disposition
- 1 September 1996
Inhibition studies showed that MDZ hydroxylation was strongly inhibited by ketoconazole and Ro 23-7637 in rat, human, and cDNA-expressed human CYP3A4 microsomes, thus suggesting that members of the CYP 3A4 subfamily were involved in the metabolism.
Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms.
Many human CYP isoforms are involved in the oxidative metabolism of 17beta-estradiol and estrone, with a varying degree of catalytic activity and distinct regioselectivity.
Cytochrome P450 enzymes involved in acetaminophen activation by rat and human liver microsomes and their kinetics.
Using this approach, involvement of enzymes in the activation of APAP and their kinetics were studied and substantial activity was observed in rat liver microsomes and human P450s expressed in Hep G2 cells.
Role of NF-kappaB in regulation of PXR-mediated gene expression: a mechanism for the suppression of cytochrome P-450 3A4 by proinflammatory agents.
It is reported that NF-kappaB activation by lipopolysaccharide and tumor necrosis factor-alpha plays a pivotal role in the suppression of cyp3a4 through interactions of NF-KappaB with the PXR, and NF- kappaB p65 directly interacted with the DNA-binding domain of RXRalpha and may prevent its binding to the consensus DNA sequences, thus inhibiting the transactivation by the PxR.
Methoxyresorufin and benzyloxyresorufin: substrates preferentially metabolized by cytochromes P4501A2 and 2B, respectively, in the rat and mouse.
PCBs: structure–function relationships and mechanism of action
There was an excellent correlation between AHH induction potencies and receptor binding avidities of these compounds and the order of activity was coplanar PCBs, the halogenated aromatic hydrocarbons which exhibit the highest binding affinities for the receptor protein.
Regulation of two members of the steroid-inducible cytochrome P450 subfamily (3A) in rats.
The studies show that constitutive expression and induction of steroid-inducible cytochrome P450s may vary as a function of age.
Characterization of a major form of rat hepatic microsomal cytochrome P-450 induced by isoniazid.
Effects of phenethyl isothiocyanate, a carcinogenesis inhibitor, on xenobiotic-metabolizing enzymes and nitrosamine metabolism in rats.
The study demonstrates that PEITC selectively affects xenobiotic-metabolizing enzymes in the liver, lung and nasal mucosa and it is especially effective in inhibiting the P450-dependent oxidation of NNK in the lung and of NDMA in the Liver.