Acquired resistance to BRAF inhibition can confer cross-resistance to combined BRAF/MEK inhibition.

@article{Gowrishankar2012AcquiredRT,
  title={Acquired resistance to BRAF inhibition can confer cross-resistance to combined BRAF/MEK inhibition.},
  author={Kavitha Gowrishankar and Stephanie Snoyman and Gulietta M. Pupo and Therese M. Becker and Richard F. Kefford and Helen Rizos},
  journal={The Journal of investigative dermatology},
  year={2012},
  volume={132 7},
  pages={1850-9}
}
Aberrant activation of the BRAF kinase occurs in ∼60% of melanomas, and although BRAF inhibitors have shown significant early clinical success, acquired resistance occurs in most patients. Resistance to chronic BRAF inhibition often involves reactivation of mitogen-activated protein kinase (MAPK) signaling, and the combined targeting of BRAF and its downstream target MAPK/ERK kinase (MEK) may delay or overcome resistance. To investigate the efficacy of combination BRAF and MEK inhibition, we… CONTINUE READING

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Selective inhibition of oncogenic BRAF V 600 E / K / D by GSK 2118436 : evidence of clinical activity in subjects with metastatic melanoma

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