Biochemical correlates of mTOR inhibition by the rapamycin ester CCI-779 and tumor growth inhibition.

@article{Dudkin2001BiochemicalCO,
  title={Biochemical correlates of mTOR inhibition by the rapamycin ester CCI-779 and tumor growth inhibition.},
  author={Lorina Dudkin and Michael B. Dilling and Pamela J. Cheshire and Franklin C. Harwood and Melinda G. Hollingshead and Susan G. Arbuck and Robert Travis and Edward A. Sausville and Peter James Houghton},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  year={2001},
  volume={7 6},
  pages={1758-64}
}
The rapamycin ester, CCI-779, potently inhibits cell growth in vitro, inhibits tumor growth in vivo, and is currently in Phase I clinical trials. To further understand the relationship between plasma systemic exposure and inhibition of the target Ser/Thr kinase, mTOR/FRAP, two assays have been developed. The first assay involves determination of the 4E suppressor protein (4E-BP1) bound to eukaryotic initiation factor 4E (eIF4E), and the second is direct Western analysis of phosphorylation of… CONTINUE READING

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Acquired resistance to rapamycin is mediated by altered regulation of the 4EBP1/eIF4E pathway

  • M. B. Dilling, G. S. Germain, P. J. Houghton
  • Proc. Am. Assoc. Cancer Res.,
  • 2000
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