RasGRPs Are Targets of the Anti-Cancer Agent Ingenol-3-Angelate

  title={RasGRPs Are Targets of the Anti-Cancer Agent Ingenol-3-Angelate},
  author={Xiaohua Song and Ana Lopez-Campistrous and Lucy Sun and Nancy A. Dower and Noemi Kedei and Jing Yang and Jessica S. Kelsey and Nancy E. Lewin and Tim E. Esch and Peter M. Blumberg and James C. Stone},
  booktitle={PloS one},
Ingenol-3-angelate (I3A) is a non-tumor promoting phorbol ester-like compound identified in the sap of Euphoria peplus. Similar to tumor promoting phorbol esters, I3A is a diacylglycerol (DAG) analogue that binds with high affinity to the C1 domains of PKCs, recruits PKCs to cellular membranes and promotes enzyme activation. Numerous anti-cancer activities have been attributed to I3A and ascribed to I3A's effects on PKCs. We show here that I3A also binds to and activates members of the RasGRP… CONTINUE READING
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