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Research ArticleArticle

Catalytic Activities of Tumor-Specific Human Cytochrome P450 CYP2W1 Toward Endogenous Substrates

Yan Zhao, Debin Wan, Jun Yang, Bruce D. Hammock and Paul R. Ortiz de Montellano
Drug Metabolism and Disposition May 2016, 44 (5) 771-780; DOI: https://doi.org/10.1124/dmd.116.069633
Yan Zhao
Department of Pharmaceutical Chemistry, University of California, San Francisco (Y.Z., P.R.O.M.) and Department of Entomology and Cancer Center, University of California, Davis, CA (D.W., J.Y., B.D.H.)
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Debin Wan
Department of Pharmaceutical Chemistry, University of California, San Francisco (Y.Z., P.R.O.M.) and Department of Entomology and Cancer Center, University of California, Davis, CA (D.W., J.Y., B.D.H.)
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Jun Yang
Department of Pharmaceutical Chemistry, University of California, San Francisco (Y.Z., P.R.O.M.) and Department of Entomology and Cancer Center, University of California, Davis, CA (D.W., J.Y., B.D.H.)
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Bruce D. Hammock
Department of Pharmaceutical Chemistry, University of California, San Francisco (Y.Z., P.R.O.M.) and Department of Entomology and Cancer Center, University of California, Davis, CA (D.W., J.Y., B.D.H.)
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Paul R. Ortiz de Montellano
Department of Pharmaceutical Chemistry, University of California, San Francisco (Y.Z., P.R.O.M.) and Department of Entomology and Cancer Center, University of California, Davis, CA (D.W., J.Y., B.D.H.)
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Abstract

CYP2W1 is a recently discovered human cytochrome P450 enzyme with a distinctive tumor-specific expression pattern. We show here that CYP2W1 exhibits tight binding affinities for retinoids, which have low nanomolar binding constants, and much poorer binding constants in the micromolar range for four other ligands. CYP2W1 converts all-trans retinoic acid (atRA) to 4-hydroxy atRA and all-trans retinol to 4-OH all-trans retinol, and it also oxidizes retinal. The enzyme much less efficiently oxidizes 17β-estradiol to 2-hydroxy-(17β)-estradiol and farnesol to a monohydroxylated product; arachidonic acid is, at best, a negligible substrate. These findings indicate that CYP2W1 probably plays an important role in localized retinoid metabolism that may be intimately linked to its involvement in tumor development.

Footnotes

    • Received January 25, 2015.
    • Accepted February 29, 2016.
  • This research was supported by National Institutes of Health National Institute of General Medical Sciences [Grant GM25515], the National Institute of Environmental Health Sciences [Grant R01 EX002710 and P42 Superfund Program], and the West Coast Central Comprehensive Metabolomic Research Core [U24 DK097154].

  • dx.doi.org/10.1124/dmd.116.069633.

  • ↵Embedded ImageThis article has supplemental material available at dmd.aspetjournals.org.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 44 (5)
Drug Metabolism and Disposition
Vol. 44, Issue 5
1 May 2016
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Research ArticleArticle

CYP 2W1 Endogenous Substrates

Yan Zhao, Debin Wan, Jun Yang, Bruce D. Hammock and Paul R. Ortiz de Montellano
Drug Metabolism and Disposition May 1, 2016, 44 (5) 771-780; DOI: https://doi.org/10.1124/dmd.116.069633

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Research ArticleArticle

CYP 2W1 Endogenous Substrates

Yan Zhao, Debin Wan, Jun Yang, Bruce D. Hammock and Paul R. Ortiz de Montellano
Drug Metabolism and Disposition May 1, 2016, 44 (5) 771-780; DOI: https://doi.org/10.1124/dmd.116.069633
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