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December 18, 1989FEBS LettersOpen Access

Potent selective inhibitors of protein kinase C

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Authors

PDPeter D. DavisUniversity of North Carolina at Chapel HillCHChristopher H. HillRoosevelt UniversityEKElizabeth KeechRoche (United Kingdom)

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Implication

Experimental study demonstrates selective protein kinase C inhibition in platelets and T cells, indicating potential immunosuppressive therapeutic utility.

Key Points

  • To develop potent and selective inhibitors of protein kinase C based on the structural leads provided by staurosporine and K252a.
  • Derived a series of selective inhibitor analogues using staurosporine and K252a structural templates.
  • Tested inhibitory efficacy in intact cellular systems, including platelets and T cells.
  • Assayed cellular proliferation in mononuclear cells stimulated with interleukin 2.
  • Novel compounds potently and selectively blocked protein kinase C activity in intact platelets and T cells.
  • Inhibitors prevented the proliferation of mononuclear cells in response to interleukin 2.

Cite This Study

Davis et al. (1989) studied this question.

synapsesocial.com/papers/6a77728c4fe2e6ffd8ecada8https://doi.org/10.1016/0014-5793(89)81494-2
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Also Consider

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  1. 1Analysis of phosphate metabolites, the intracellular pH, and the state of adenosine triphosphate in intact muscle by phosphorus nuclear magnetic resonance.1976 · 341 citations
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  3. 3Purification and characterization of a calmodulin-dependent kinase from rat brain cytosol able to phosphorylate tubulin and microtubule-associated proteins.1983 · 342 citations