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Conformationally constrained analogues of diacylglycerol. 29. Cells sort diacylglycerol-lactone chemical zip codes to produce diverse and selective biological activities

  1. Author:
    Duan, D.
    Sigano, D. M.
    Kelley, J. A.
    Lai, C. C.
    Lewin, N. E.
    Kedei, N.
    Peach, M. L.
    Lee, J.
    Abeyweera, T. P.
    Rotenberg, S. A.
    Kim, H.
    Kim, Y. H.
    El Kazzouli, S.
    Chung, J. U.
    Young, H. A.
    Young, M. R.
    Baker, A.
    Colburn, N. H.

  2. Author Address

    Duan, Dehui, Sigano, Dina M.; Kelley, James A.; Lai, Christopher C.; El Kazzouli, Said, Marquez, Victor E.] NCI, NIH, Med Chem Lab, Frederick, MD 21702 USA. [Lewin, Nancy E.; Kedei, Noemi, Perry, Nicholas A.; Surawski, Robert J.; Blumberg, Peter M.] NCI, NIH, Lab Canc Biol & Genet, Bethesda, MD 20892 USA. [Peach, Megan L.] Basic Res Program SAIC Frederick Inc, NCI Frederick, Frederick, MD 21702 USA. [Lee, Jeewoo, Chung, Jae-Uk] Seoul Natl Univ, Coll Pharm, Res Inst Pharmaceut Sci, Med Chem Lab, Seoul 151742, South Korea. [Duan, Dehui, Abeyweera, Thushara P.; Rotenberg, Susan A.] CUNY Queens Coll, Dept Chem & Biochem, Flushing, NY 11367 USA. [Kim, Young Ho] Digital Biotech, Ansa Si 425839, Kyonggi Do, South Korea. [Young, Howard A.] NCI, NIH, Expt Immunol Lab, Frederick, MD 21702 USA. [Young, Matthew R.; Baker, Alyson, Colburn, Nancy H.] NCI, NIH, Lab Canc Prevent, Frederick, MD 21702 USA. [Haimovitz-Friedman, Adriana, Truman, Jean-Philip] Mem Sloan Kettering Canc Ctr, Dept Radiat Oncol, New York, NY 10021 USA. [Parrish, Damon A.; Deschamps, Jeffrey R.] USN, Res Lab, Washington, DC 20375 USA.
    1. Year: 2008
  2. Journal: Journal of Medicinal Chemistry
    1. 51
    2. 17
    3. Pages: 5198-5220
  4. Type of Article: Article
  1. Abstract:

    Diacylglycerol-lactone (DAG-lactone) libraries generated by a solid-phase approach using IRORI technology produced a variety of unique biological activities. Subtle differences in chemical diversity in two areas of the molecule, the combination of which generates what we have termed "chemical zip codes", are able to transform a relatively small chemical space into a larger universe of biological activities, as membrane-containing organelles within the cell appear to be able to decode these "chemical zip codes". It is postulated that after binding to protein kinase C (PKC) isozymes or other nonkinase target proteins that contain diacylglycerol responsive, membrane interacting domains (C1 domains), the resulting complexes are directed to diverse intracellular sites where different sets of substrates are accessed. Multiple cellular bioassays show that DAG-lactones, which bind in vitro to PKC alpha to varying degrees, expand their biological repertoire into a larger domain, eliciting distinct cellular responses.

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External Sources

  1. PMID: 18698758

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