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Role of furanocoumarin derivatives on grapefruit juice-mediated inhibition of human CYP3A activity.
TLDR
All six furanocoumarins showed stronger CYP3A inhibitory potencies after preincubation in the presence of NADPH, suggesting that both competitive and mechanism-based inhibition occur in a grapefruit juices-drug interaction. Expand
Inhibition selectivity of grapefruit juice components on human cytochromes P450.
TLDR
Furanocoumarin dimers, GF-I-1 and GF-i-4, were the most potent inhibitors of CYP3A4, suggesting that these compounds are mechanism-based inhibitors of cytochrome P450 (P450) forms. Expand
Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole.
TLDR
The results indicate the involvement of CYP2J2 in the presystemic elimination of astemizole in the human small intestine, since P450 included in this subfamily is dominantly expressed in the small intestine of rabbits. Expand
Role of human hepatocyte nuclear factor 4alpha in the expression of drug-metabolizing enzymes and transporters in human hepatocytes assessed by use of small interfering RNA.
TLDR
It is suggested that H NF4alpha plays a dominant role in the expression of drug-metabolizing enzymes and transporters in human hepatocytes, and that HNF4alpha expression levels is a possible determinant for inter-individual variations in theexpression of these enzymes andtransporters. Expand
Protective Role of Hydroxysteroid Sulfotransferase in Lithocholic Acid-induced Liver Toxicity*
TLDR
Results indicate hydroxysteroid sulfotransferase-mediated LCA sulfation as a major pathway for protection against LCA-induced liver damage. Expand
A new cytochrome P450 form belonging to the CYP2D in dog liver microsomes: purification, cDNA cloning, and enzyme characterization.
TLDR
Western blot analysis suggested that P450 DUT2 is a constitutive and major (approximately 20% of the total P450) form, indicating that the 2D subfamily P450 in dog liver is quite unique from CYP2D members of other species. Expand
Isolation and Characterization of a New Major Intestinal CYP3A Form, CYP3A62, in the Rat
TLDR
Despite clear detection of CYP3A62, no detectable levels of CYp3A1 and CYP4A2 proteins, as well as those of mRNAs, were found in the intestinal tract, therefore, CYP 3A62 may play major roles together with CYP2A9 and CYB3A18 in endogenous or exogenous detoxification at the absorption site. Expand
A Common Regulatory Region Functions Bidirectionally in Transcriptional Activation of the Human CYP1A1 and CYP1A2 Genes
TLDR
In the present study, a reporter gene construct containing -22.4 kb of the 5′-flanking region of the CYP1A2 gene was found to support β-naphthoflavone (BNF) and 3-methylchoranthrene (3-MC)-mediated transcriptional activation, establishing that induction of human CYP 1A1 and CYP2 is simultaneously controlled through bidirectional and common regulatory elements. Expand
Phenol sulfotransferase, ST1A3, as the main enzyme catalyzing sulfation of troglitazone in human liver.
TLDR
Accumulation of unmetabolized troglitazone causes the cytotoxicity in the hepatoma cells and may be responsible for toxicity in human liver. Expand
Specific CYP3A4 inhibitors in grapefruit juice: furocoumarin dimers as components of drug interaction.
TLDR
These furocoumarins are strong candidates for causative agents of grapefruit juice-mediated drug interaction, because of an inhibition potential that is equal to or stronger than the prototypical CYP3A4 inhibitor, ketoconazole, on liver microsomal testosterone 6 beta-hydroxylation. Expand
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