Preclinical Development Combinations of BRAF , MEK , and PI 3 K / mTOR Inhibitors Overcome Acquired Resistance to the BRAF Inhibitor GSK 2118436 Dabrafenib , Mediated by NRAS or MEK Mutations

@inproceedings{Greger2012PreclinicalDC,
  title={Preclinical Development Combinations of BRAF , MEK , and PI 3 K / mTOR Inhibitors Overcome Acquired Resistance to the BRAF Inhibitor GSK 2118436 Dabrafenib , Mediated by NRAS or MEK Mutations},
  author={James G. Greger and Stephen D. Eastman and Vivian Z Zhang and Maureen R. Bleam and Ashley M. Hughes and Kimberly N. Smitheman and Scott H. Dickerson and Sylvie G. Laquerre and Li Liu and Tona M. Gilmer},
  year={2012}
}
Recent results from clinical trials with the BRAF inhibitors GSK2118436 (dabrafenib) and PLX4032 (vemurafenib) have shown encouraging response rates; however, the duration of response has been limited. To identify determinants of acquired resistance to GSK2118436 and strategies to overcome the resistance, we isolated GSK2118436 drug-resistant clones from the A375 BRAF and the YUSIT1 BRAF melanoma cell lines. These clones also showed reduced sensitivity to the allosteric mitogen-activated… CONTINUE READING
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Phase I/II study of GSK2118436, a selective inhibitor of oncogenic mutant BRAF kinase, in patients with metastatic melanoma and other solid tumors

  • R Kefford, H Arkenau, MP Brown, M Millward, JR Infante, GV Long
  • ASCO Meeting Abstracts
  • 2010
Highly Influential
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