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Synthesis and Biological Evaluation of Fluorescent Bryostatin Analogues

  1. Author:
    Cummins, Thomas J.
    Kedei, Noemi
    Czikora, Agnes
    Lewin, Nancy E.
    Kirk, Sharon
    Petersen, Mark E.
    McGowan, Kevin M.
    Chen, Jin-Qiu
    Luo, Xiaoling
    Johnson, Randall
    Ravichandran, Ravi
    Blumberg, Peter M.
    Keck, Gary E.

  2. Author Address

    NCI, Lab Canc Biol & Genet, Ctr Canc Res, 37 Convent Dr,Room 4048, Bethesda, MD 20892 USA.Univ Utah, Dept Chem, 315 South 1400 East,Room 2020, Salt Lake City, UT 84112 USA.NCI, Collaborat Prot Technol Resource, Ctr Canc Res, 37 Convent Dr,Room 1044, Bethesda, MD 20892 USA.Leidos Biomed Res Inc, Adv Biomed & Computat Sci Biomed Informat & Data, Directorate Frederick Natl Lab Canc Res FNLCR, Bldg 430,Miller Dr, Frederick, MD 21702 USA.
    1. Year: 2018
    2. Date: Apr 16
  2. Journal: Chembiochem
  3. WILEY-V C H VERLAG GMBH,
    1. 19
    2. 8
    3. Pages: 877-889
  5. Type of Article: Article
  6. ISSN: 1439-4227
  1. Abstract:

    To investigate the cellular distribution of tumor-promoting vs. non-tumor-promoting bryostatin analogues, we synthesized fluorescently labeled variants of two bryostatin derivatives that have previously shown either phorbol ester-like or bryostatin-like biological activity in U937 leukemia cells. These new fluorescent analogues both displayed high affinity for protein kinaseC (PKC) binding and retained the basic properties of the parent unlabeled compounds in U937 assays. The fluorescent compounds showed similar patterns of intracellular distribution in cells, however; this argues against an existing hypothesis that various patterns of intracellular distribution are responsible for differences in biological activity. Upon further characterization, the fluorescent compounds revealed a slow rate of cellular uptake; correspondingly, they showed reduced activity for cellular responses that were only transient upon treatment with phorbol ester or bryostatin1.

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External Sources

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  2. DOI: 10.1002/cbic.201700655
  3. PMID: 29424951
  4. View record in Web of Science®
  5. WOS: 000430168000015

Library Notes

  1. Fiscal Year: FY2017-2018
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