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Center for Nephrology and Metabolic Disorders
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Cytochrome P450 3A4

The CYP3A4 gene encodes an enzyme from the cytochrome P450 superfamily which is involved in metabolism of steroids (hormones and lipids) and various drugs.

Interpretation

CYP3A4 inhibitors

Antiarrhythmics Dronedaron

Antibiotics Erythromycin, Clarithromycin, Telithromycin

Antidepressants Nefazodon

Antimycotic drugs Itraconazol, Ketoconazol, Voriconazol

Protease inhibitors Indinavir, Nelfinavir, Ritonavir

Cytostatics Idelalisib, Ribocuclib

Other Grapefruitesaft

CYP3A4 inducer

Antibiotics Rifampicin

Antidiabetics Pioglitazon

Anticonvulsants Carbamazepin, Oxcarbazepin, Phenytoin

Antiretroviral drugs Efavirenz, Nevirapin

Glucocorticoids

Cytostatics Brigatinib, Enzalutamid

Tranquillizers Barbiturate, Phenobarbital

Other Hypericum, Modafinil

Genetests:

Clinic Method Carrier testing
Turnaround 5 days
Specimen type genomic DNA
Clinic Method Massive parallel sequencing
Turnaround 25 days
Specimen type genomic DNA
Research Method Genomic sequencing of the entire coding region
Turnaround 25 days
Specimen type genomic DNA
Research Method Multiplex Ligation-Dependent Probe Amplification
Turnaround 25 days
Specimen type genomic DNA

Related Diseases:

Disturbances of cytochrome p450 system
CYP1A2
CYP2A6
CYP2C9
CYP2D6
CYP3A4
CYP4F2
Siponimod intolerance
CYP2C9

References:

1.

Dimaraki EV et al. (2003) Troglitazone induces CYP3A4 activity leading to falsely abnormal dexamethasone suppression test.

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2.

Lehmann JM et al. (1998) The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.

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3.

Felix CA et al. (1998) Association of CYP3A4 genotype with treatment-related leukemia.

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4.

Paris PL et al. (1999) Association between a CYP3A4 genetic variant and clinical presentation in African-American prostate cancer patients.

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5.

Goodwin B et al. (1999) The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module.

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6.

Walker AH et al. (1998) Characterization of an allelic variant in the nifedipine-specific element of CYP3A4: ethnic distribution and implications for prostate cancer risk. Mutations in brief no. 191. Online.

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7.

Xie W et al. (2000) Humanized xenobiotic response in mice expressing nuclear receptor SXR.

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8.

Kittles RA et al. (2002) CYP3A4-V and prostate cancer in African Americans: causal or confounding association because of population stratification?

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9.

Goodwin B et al. (2002) Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor.

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10.

Zeigler-Johnson CM et al. (2002) Ethnic differences in the frequency of prostate cancer susceptibility alleles at SRD5A2 and CYP3A4.

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11.

Tirona RG et al. (2003) The orphan nuclear receptor HNF4alpha determines PXR- and CAR-mediated xenobiotic induction of CYP3A4.

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12.

Nebert DW et al. (1987) P450 genes: structure, evolution, and regulation.

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13.

Masuyama H et al. (2003) Expression and potential roles of pregnane X receptor in endometrial cancer.

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14.

Markowitz JS et al. (2003) Effect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme.

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15.

Loukola A et al. (2004) Comprehensive evaluation of the association between prostate cancer and genotypes/haplotypes in CYP17A1, CYP3A4, and SRD5A2.

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16.

Gupta RP et al. (2004) CYP3A4 is a human microsomal vitamin D 25-hydroxylase.

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17.

Williams PA et al. (2004) Crystal structures of human cytochrome P450 3A4 bound to metyrapone and progesterone.

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18.

Hirota T et al. (2004) Allelic expression imbalance of the human CYP3A4 gene and individual phenotypic status.

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19.

Gupta RP et al. (2005) CYP3A4 is a vitamin D-24- and 25-hydroxylase: analysis of structure function by site-directed mutagenesis.

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20.

Schirmer M et al. (2006) Genetic signature consistent with selection against the CYP3A4*1B allele in non-African populations.

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21.

Ekroos M et al. (2006) Structural basis for ligand promiscuity in cytochrome P450 3A4.

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22.

van Herwaarden AE et al. (2007) Knockout of cytochrome P450 3A yields new mouse models for understanding xenobiotic metabolism.

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23.

Thummel KE et al. (1998) In vitro and in vivo drug interactions involving human CYP3A.

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24.

Paolini M et al. (1999) Co-carcinogenic effect of beta-carotene.

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25.

Daly AK et al. (1992) Deficient nifedipine oxidation: a rare inherited trait associated with cystic fibrosis kindreds.

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26.

Inoue K et al. (1992) Assignment of the human cytochrome P-450 nifedipine oxidase gene (CYP3A4) to chromosome 7 at band q22.1 by fluorescence in situ hybridization.

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27.

Wolf CR et al. (1992) Relationship between the debrisoquine hydroxylase polymorphism and cancer susceptibility.

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28.

Wrighton SA et al. (1992) The human hepatic cytochromes P450 involved in drug metabolism.

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29.

Forrester LM et al. (1990) Evidence for involvement of multiple forms of cytochrome P-450 in aflatoxin B1 metabolism in human liver.

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30.

Shimada T et al. (1989) Evidence for cytochrome P-450NF, the nifedipine oxidase, being the principal enzyme involved in the bioactivation of aflatoxins in human liver.

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31.

Wrighton SA et al. (1989) Isolation and characterization of human fetal liver cytochrome P450HLp2: a third member of the P450III gene family.

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32.

Spurr NK et al. (1989) The human cytochrome P450 CYP3 locus: assignment to chromosome 7q22-qter.

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33.

Brooks BA et al. (1988) The gene CYP3 encoding P450pcn1 (nifedipine oxidase) is tightly linked to the gene COL1A2 encoding collagen type 1 alpha on 7q21-q22.1.

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34.

Renwick AG et al. (1988) The pharmacokinetics of oral nifedipine--a population study.

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35.

Gonzalez FJ et al. (1988) Human P450PCN1: sequence, chromosome localization, and direct evidence through cDNA expression that P450PCN1 is nifedipine oxidase.

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36.

Schellens JH et al. (1988) Lack of bimodality in nifedipine plasma kinetics in a large population of healthy subjects.

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37.

Molowa DT et al. (1986) Complete cDNA sequence of a cytochrome P-450 inducible by glucocorticoids in human liver.

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38.

Watkins PB et al. (1985) Identification of an inducible form of cytochrome P-450 in human liver.

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39.

Kleinbloesem CH et al. (1984) Variability in nifedipine pharmacokinetics and dynamics: a new oxidation polymorphism in man.

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40.

Elshourbagy NA et al. (1980) Separation, purification, and characterization of a novel form of hepatic cytochrome P-450 from rats treated with pregnenolone-16 alpha-carbonitrile.

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41.

Shet MS et al. (1993) Human cytochrome P450 3A4: enzymatic properties of a purified recombinant fusion protein containing NADPH-P450 reductase.

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42.

Chen H et al. (1996) Increased risk for myelodysplastic syndromes in individuals with glutathione transferase theta 1 (GSTT1) gene defect.

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43.

Lown KS et al. (1997) Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression.

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44.

Rebbeck TR et al. (1998) Modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4.

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45.

Orphanet article

Orphanet ID 423802 external link
46.

NCBI article

NCBI 1576 external link
47.

OMIM.ORG article

Omim 124010 external link
48.

Wikipedia article

Wikipedia EN (CYP3A4) external link
Update: Aug. 14, 2020
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