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Zebularine: A unique molecule for an epigenetically based strategy in cancer chemotherapy

  1. Author:
    Marquez, V. E.
    Kelley, J. A.
    Agbaria, R.
    Ben-Kasus, T.
    Cheng, J. C.
    Yoo, C. B.
    Jones, P. A.

  2. Author Address

    NCI, Canc Res Ctr, Med Chem Lab, NIH, Frederick, MD 21702 USA. Ben Gurion Univ Negev, Fac Hlth Sci, Dept Clin Pharmacol, IL-84105 Beer Sheva, Israel. Univ So Calif, Keck Sch Med, Norris Comprehens Canc Ctr, Dept Urol, Los Angeles, CA 90089 USA. Univ So Calif, Keck Sch Med, Norris Comprehens Canc Ctr, Dept Biochem, Los Angeles, CA 90089 USA. Univ So Calif, Keck Sch Med, Norris Comprehens Canc Ctr, Dept Biol Mol, Los Angeles, CA 90089 USA.;Marquez, VE, NCI, Canc Res Ctr, Med Chem Lab, NIH, Frederick, MD 21702 USA.;marquezv@dc37a.nci.nih.gov
    1. Year: 2005
  2. Book Title: Therapeutic Oligonucleotides: Transcriptional and Translational Strategies for Silencing Gene Expression
  3. Series Title: Annals of the New York Academy of Sciences
  4. New York Acad Sciences
  5. New York
    1. 1058
    2. Pages: 246-254
  7. Type of Work: Book Chapter
  8. ISBN: 0077-8923
  1. Abstract:

    1-(beta-D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine) corresponds structurally to cytidine minus the exocyclic 4-amino group. The increased electrophilic character of its simple aglycon endows the molecule with unique biologic properties as a potent inhibitor of both cytidine deaminase and DNA cytosine methyltransferase. The latter activity makes zebularine a promising antitumor agent that is hydrolytically stable, preferentially targets cancer cells, and shows activity both in vitro and in experimental animals, even after oral administration.

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External Sources

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  2. DOI: 10.1196/annals.1359.037
  3. View record in Web of Science®
  4. WOS: 000236466000021

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