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CHOLESTEROL-METABOLIZING CYTOCHROMES P450

Irina A. Pikuleva
Drug Metabolism and Disposition April 2006, 34 (4) 513-520; DOI: https://doi.org/10.1124/dmd.105.008789
Irina A. Pikuleva
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Abstract

By catalyzing the first steps in different pathways of cholesterol degradation, cytochromes P450 (P450s) 7A1, 27A1, 11A1, and 46A1 play key roles in cholesterol homeostasis. CYP7A1 is a microsomal liver-specific enzyme that converts cholesterol to 7α-hydroxycholesterol. CYP27A1 is a ubiquitously expressed mitochondrial P450 that metabolizes cholesterol to 27-hydroxycholesterol. CYP11A1 also resides in mitochondria but is expressed mainly in steroidogenic tissues, where it catalyzes the conversion of cholesterol to pregnenolone. Finally, CYP46A1 is a brain-selective microsomal monooxygenase producing 24S-hydroxycholesterol from cholesterol. Catalytic efficiencies of cholesterol-metabolizing P450s vary significantly and probably reflect physiological requirements of different organs for the rate of cholesterol turnover. P450s 7A1, 27A1, 11A1, and 46A1 represent a unique system for elucidation of how different enzymes have adapted to fit their specific roles in cholesterol elimination. Studies of cholesterol-metabolizing P450s suggest that their activities could be modulated post-translationally and that they should also be considered as targets for regulation of cholesterol homeostasis.

Footnotes

  • Studies in the author's laboratory described in this paper are supported by National Institutes of Health Grants GM62882 and AG024336.

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

  • doi:10.1124/dmd.105.008789.

  • ABBREVIATIONS: P450, cytochrome P450 enzyme; LDL, low-density lipoprotein; LXR, liver X receptor; CTX, cerebrotendinous xanthomatosis; ER, endoplasmic reticulum; PL, phospholipid; SFA, saturated fatty acid; MUFA, monounsaturated fatty acid; PUFA, polyunsaturated fatty acid.

    • Received December 3, 2005.
    • Accepted January 18, 2006.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 34 (4)
Drug Metabolism and Disposition
Vol. 34, Issue 4
1 Apr 2006
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CHOLESTEROL-METABOLIZING CYTOCHROMES P450

Irina A. Pikuleva
Drug Metabolism and Disposition April 1, 2006, 34 (4) 513-520; DOI: https://doi.org/10.1124/dmd.105.008789

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CHOLESTEROL-METABOLIZING CYTOCHROMES P450

Irina A. Pikuleva
Drug Metabolism and Disposition April 1, 2006, 34 (4) 513-520; DOI: https://doi.org/10.1124/dmd.105.008789
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    • Physiological and Medical Significance of Cholesterol-Metabolizing P450s
    • Cholesterol-Metabolizing P450s as a Unique System for Investigation
    • Structure /Function Studies of Cholesterol-Metabolizing P450s
    • A Possible Strategy to Modulate Activity of Cholesterol-Metabolizing P450s
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