Antagonism of SET using OP449 enhances the efficacy of tyrosine kinase inhibitors and overcomes drug resistance in myeloid leukemia.

@article{Agarwal2014AntagonismOS,
  title={Antagonism of SET using OP449 enhances the efficacy of tyrosine kinase inhibitors and overcomes drug resistance in myeloid leukemia.},
  author={Anupriya Agarwal and Ryan J Mackenzie and Raffaella Pippa and Christopher A. Eide and Jessica Oddo and Jeffrey W. Tyner and Rosalie C. Sears and Michael P Vitek and Mar{\'i}a Dolores Odero and Dale J. Christensen and Brian J. Druker},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  year={2014},
  volume={20 8},
  pages={2092-103}
}
PURPOSE The SET oncoprotein, a potent inhibitor of the protein phosphatase 2A (PP2A), is overexpressed in leukemia. We evaluated the efficacy of SET antagonism in chronic myeloid leukemia (CML) and acute myeloid leukemia (AML) cell lines, a murine leukemia model, and primary patient samples using OP449, a specific, cell-penetrating peptide that antagonizes SET's inhibition of PP2A. EXPERIMENTAL DESIGN In vitro cytotoxicity and specificity of OP449 in CML and AML cell lines and primary samples… CONTINUE READING
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