CYP3A4

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CYP3A4

A gene on chromosome 7q21.1 that encodes a member of the cytochrome P450 superfamily of monooxygenases, which catalyse reactions in drug metabolism and synthesis of cholesterol, steroids and other lipids. CYP3A4 localises to the endoplasmic reticulum; its expression is induced by glucocorticoids and drugs. It metabolises roughly half of the drugs in current use today—e.g., paracetamol (acetaminophen), codeine, cyclosporin A, diazepam and erythromycin—as well as steroids and carcinogens.

CYP3A4

One isoenzyme form of the cytochrome P450 system involved in the metabolism of many drugs. Drugs that alter this enzyme system can influence the metabolism of other agents taken by patients and cause unanticipated toxic effects.
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The human CYP3A subfamily consists of four Known members - CYP3A4, 3A5, 3A7 and 3A43 (Lamba et al.
Investigation of cytochrome P450 1A2 and 3A inhibitory properties of Danshen tincture
The subtypes of CYP enzymes tested for were: ethoxyresorufin O-de-ethylase, CYPIA1; methoxyresorufin O-demethylase, CYPIA2; pentoxyresorufin O-dealkylase, CYP2B; (S)-warfarin 7-hydroxyIase, CYP2C; p-nitrophenol hydroxylase, CYP2E1; and testosterone 6[beta]-hydroxylase, CYP3A.
Ginkgo biloba extract attenuates warfarin-mediated anticoagulation through induction of hepatic cytochrome p450 enzymes by bilobalide in mice
The CYP3A subfamily in humans comprises the 3A3, 3A4, and 3A5 isoenzymes in adults and the 3A7 isoenzyme in fetal liver.
Pharmacogenetics: a laboratory tool for optimizing therapeutic efficiency
1993) suggested that CYP2B6, CYP2C9 and CYP3A may be affected in vivo.
Polysaccharide peptides from Coriolus versicolor competitively inhibit tolbutamide 4-hydroxylation in specific human CYP2C9 isoform and pooled human liver microsomes
Assessment of the hepatic and intestinal first-pass metabolism of midazolam in a CYP3A drug-drug interaction model rats.
Major tanshinones of Danshen (Salvia miltiorrhiza) exhibit different modes of inhibition on human CYP1A2, CYP2C9, CYP2E1 and CYP3A4 activities in vitro
This study investigated the effect of Danshen on the pharmacodynamic-pharmacokinetic (PD-PK) effects of midazolam, a model CYP3A probe substrate.
A pharmacodynamic-pharmacokinetic (PD-PK) study on the effects of Danshen (Salvia miltiorrhiza) on midazolam, a model CYP3A probe substrate, in the rat
2006) suggested possible induction of CYP3A by tanshinone IIA.
Pharmacokinetic interaction studies of tanshinones with tolbutamide, a model CYP2C11 probe substrate, using liver microsomes, primary hepatocytes and in vivo in the rat
The relative abundance and significance of individual CYP enzyme in human drug metabolism varies, the more important CYP isoform families include CYP1A, CYP2C, CYP2D and CYP3A.
Effects of major tanshinones isolated from Danshen (salvia miltiorrhiza) on rat CYP1A2 expression and metabolism of model CYP1A2 probe substrates
Phosphorylation and protein-protein interactions in PXR-mediated CYP3A repression.
Hepatic Cyp1a2 Expression Reduction during Inflammation Elicited in a Rat Model of Intermittent Hypoxia
CYP3A variation and the evolution of salt-sensitivity variants.
Genetic signature of strong recent positive selection at interleukin-32 gene in goat
CYP3A members are the most abundant CYPs in rat and human liver and small intestine (4, 5).
The Role of Cytochrome P450 3A5 Enzyme on the Metabolism of Tacrolimus in Rats
Wang D, Sadee W (2012) The Making of a CYP3A Biomarker Panel for Guiding Drug Therapy.
Insilco modeling of commonly occurring genetic polymorphism of human cyp3a4 on the binding affinity to UR-144

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