Selective inhibition of phosphatidylinositol phospholipase C by cytotoxic ether lipid analogues.

  title={Selective inhibition of phosphatidylinositol phospholipase C by cytotoxic ether lipid analogues.},
  author={Garth Powis and Margret Seewald and Catherine Gratas and Deborah C. Melder and J F Riebow and Edward J. Modest},
  journal={Cancer research},
  volume={52 10},
The ether lipid analogue 1-octadecyl-2-methyl-rac-glycero-3-phosphocholine (ET-18-OCH3) has been shown to be a direct inhibitor of Swiss 3T3 fibroblast and BG1 ovarian adenocarcinoma cell cytosolic phosphoinositide selective phospholipase C (PIPLC) using [3H]-phosphatidylinositol-(4, 5)-bisphosphate ([3H]PIP2) as the substrate. The inhibition occurred when ET-18-OCH3 was incorporated into the [3H]PIP2 substrate micelles, with 50% inhibition (IC50) occurring at a ET-18-OCH3: [3H]PIP2 ratio of 0… CONTINUE READING
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