Characterization of the interaction of ingenol 3-angelate with protein kinase C.

  title={Characterization of the interaction of ingenol 3-angelate with protein kinase C.},
  author={Noemi Kedei and Daniel J. Lundberg and Attila L. T{\'o}th and Peter Welburn and S. H. Garfield and Peter M. Blumberg},
  journal={Cancer research},
  volume={64 9},
Ingenol 3-angelate (I3A) is one of the active ingredients in Euphorbia peplus, which has been used in traditional medicine. Here, we report the initial characterization of I3A as a protein kinase C (PKC) ligand. I3A bound to PKC-alpha in the presence of phosphatidylserine with high affinity; however, under these assay conditions, little PKC isoform selectivity was observed. PKC isoforms did show different sensitivity and selectivity for down-regulation by I3A and phorbol 12-myristate 13-acetate… CONTINUE READING


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