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Review ArticleMINIREVIEW

CYP3A Regulation: From Pharmacology to Nuclear Receptors

Linda C. Quattrochi and Philip S. Guzelian
Drug Metabolism and Disposition May 2001, 29 (5) 615-622;
Linda C. Quattrochi
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Philip S. Guzelian
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Abstract

Among the human liver cytochrome P450s (P450s), a family of microsomal hemoproteins responsible for catalyzing the oxidative metabolism of clinically used drugs and environmental chemicals, attention has been focused on CYP3A, a form that is the most abundant and is inducible by many of its substrates. From early pharmacological studies that demonstrated induction of CYP3A by glucocorticoids and, paradoxically, by antiglucocorticoids, the existence of a nonclassical glucocorticoid receptor mechanism was inferred and prompted research that culminated in the identification of a unique member of the nuclear receptor family, the pregnane X receptor (PXR; NR1I2). It has become increasingly evident that PXR as well as other nuclear receptors mediate CYP3A induction in a unique and complex manner including inducibility by structurally diverse compounds and striking interspecies differences in induction profiles. Future understanding of the role of nuclear receptors in regulating expression of CYP3A and other genes of the P450 family offers an exciting promise of further defining the physiologic function and interindividual differences of CYP3A in health and disease.

Footnotes

  • Send reprint requests to: Dr. Linda C. Quattrochi, UCHSC B-146, 4200 E. 9th Avenue, Denver, CO 80262. E-mail:linda.quattrochi{at}uchsc.edu

  • This work was supported by United States Public Health Service Grant ES05744.

  • ↵2 The sequence of the 5′-noncoding region of the rat genomic clone used in previous studies referred to as CYP3A1 is completely identical to that of the recently isolated CYPRL33 (Komori and Oda, 1994). This gene, inducible by Dex, PCN, and phenobarbital, has been assigned the name CYP3A23 (Nelson et al., 1996).

  • Abbreviations used are::
    P450
    cytochrome P450
    CAR
    constitutive androstane receptor
    COUP-TF
    chicken ovalbumin upstream promoter transcription factor
    CTZ
    clotrimazole
    Dex
    dexamethasone
    GC
    glucocorticoids
    GR
    glucocorticoid receptor
    GRE
    glucocorticoid response element
    HNF
    hepatocyte nuclear factor
    LBD
    ligand binding domain
    PB
    phenobarbital
    PBREM
    PB response element module
    PCN
    pregnenolone 16α-carbonitrile
    PXR
    pregnane X receptor
    RIF
    rifampicin
    RXR
    retinoid acid X receptor
    SXR
    steroid and xenobiotic receptor
    XREM
    xenobiotic responsive element module
    • Received October 27, 2000.
    • Accepted February 12, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 29 (5)
Drug Metabolism and Disposition
Vol. 29, Issue 5
1 May 2001
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Review ArticleMINIREVIEW

CYP3A Regulation: From Pharmacology to Nuclear Receptors

Linda C. Quattrochi and Philip S. Guzelian
Drug Metabolism and Disposition May 1, 2001, 29 (5) 615-622;

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Review ArticleMINIREVIEW

CYP3A Regulation: From Pharmacology to Nuclear Receptors

Linda C. Quattrochi and Philip S. Guzelian
Drug Metabolism and Disposition May 1, 2001, 29 (5) 615-622;
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    • Abstract
    • Inducibility of CYP3A Gene Expression
    • Characterization of the CYP3A Promoter
    • Species-Specific Induction of CYP3A Gene Expression
    • PXR and Its Role in Species-Specific Induction of CYP3A
    • Mechanisms: PXR, CAR, GR, and Others
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