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Actin is the primary cellular receptor of bistramide A

  1. Author:
    Statsuk, A. V.
    Bai, R. L.
    Baryza, J. L.
    Verma, V. A.
    Hamel, E.
    Wender, P. A.
    Kozmin, S. A.

  2. Author Address

    Univ Chicago, Dept Chem, Chicago, IL 60637 USA. NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. Stanford Univ, Dept Chem, Stanford, CA 94305 USA. Stanford Univ, Dept Mol Pharmacol, Stanford, CA 94305 USA Kozmin, SA, Univ Chicago, Dept Chem, 5735 S Ellis Ave, Chicago, IL 60637 USA
    1. Year: 2005
    2. Date: DEC
  2. Journal: Nature Chemical Biology
    1. 1
    2. 7
    3. Pages: 383-388
  4. Type of Article: Article
  1. Abstract:

    Bistramide A ( 1) is a marine natural product with broad, potent antiproliferative effects(1-7). Bistramide A has been reported to selectively activate protein kinase C (PKC) delta, leading to the view that PKC delta is the principal mediator of antiproliferative activity of this natural product(8). Contrary to this observation, we established that bistramide A binds PKCd with low affinity, does not activate this kinase in vitro and does not translocate GFP- PKCd. Furthermore, we identified actin as the cellular receptor of bistramide A. We report that bistramide A disrupts the actin cytoskeleton, inhibits actin polymerization, depolymerizes filamentous F-actin in vitro and binds directly to monomeric G-actin in a 1:1 ratio with a K-d of 7 nM. We also constructed a fully synthetic(9) bistramide A - based affinity matrix and isolated actin as a specific bistramide A - binding protein. This activity provides a molecular explanation for the potent antiproliferative effects of bistramide A, identifying it as a new biochemical tool for studies of the actin cytoskeleton and as a potential lead for development of a new class of antitumor agents(7,10)

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  2. WOS: 000233447700010

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