Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy.

@article{Stratikopoulos2015KinaseAB,
  title={Kinase and BET Inhibitors Together Clamp Inhibition of PI3K Signaling and Overcome Resistance to Therapy.},
  author={Elias E Stratikopoulos and Meaghan S. Dendy and Matthias J. Szabolcs and Alan J Khaykin and C{\'e}line Lefebvre and Ming-Ming Zhou and Ramon E. Parsons},
  journal={Cancer cell},
  year={2015},
  volume={27 6},
  pages={837-51}
}
Unsustained enzyme inhibition is a barrier to targeted therapy for cancer. Here, resistance to a class I PI3K inhibitor in a model of metastatic breast cancer driven by PI3K and MYC was associated with feedback activation of tyrosine kinase receptors (RTKs), AKT, mTOR, and MYC. Inhibitors of bromodomain and extra terminal domain (BET) proteins also failed to affect tumor growth. Interestingly, BET inhibitors lowered PI3K signaling and dissociated BRD4 from chromatin at regulatory regions of… CONTINUE READING
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