Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.

@article{King2006DemonstrationOA,
  title={Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.},
  author={Alastair J. King and Denis R. Patrick and Roberta S Batorsky and Maureen L Ho and Hieu T Do and Shu Yun Zhang and Rakesh Kumar and David W. Rusnak and Andrew K. Takle and David M Wilson and Erin D Hugger and Lifu Wang and Florian A. Karreth and Julie C Lougheed and Jae Yeung Lee and David Chau and Thomas J Stout and Earl W. May and Cynthia M Rominger and Michael D. Schaber and Lusong Luo and Ami S Lakdawala and Jerry L. Adams and Rooja G Contractor and Keiran Sm Smalley and Meenhard Herlyn and Michael M. Morrissey and David A Tuveson and Pearl S. Huang},
  journal={Cancer research},
  year={2006},
  volume={66 23},
  pages={11100-5}
}
Oncogenic BRAF alleles are both necessary and sufficient for cellular transformation, suggesting that chemical inhibition of the activated mutant protein kinase may reverse the tumor phenotype. Here, we report the characterization of SB-590885, a novel triarylimidazole that selectively inhibits Raf kinases with more potency towards B-Raf than c-Raf. Crystallographic analysis revealed that SB-590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration, which is distinct from… CONTINUE READING

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