Inhibitors of Ras/Raf-1 interaction identified by two-hybrid screening revert Ras-dependent transformation phenotypes in human cancer cells.

@article{KatoStankiewicz2002InhibitorsOR,
  title={Inhibitors of Ras/Raf-1 interaction identified by two-hybrid screening revert Ras-dependent transformation phenotypes in human cancer cells.},
  author={Juran Kato-Stankiewicz and Irina Hakimi and Gang Zhi and Jie Zhang and Ilya G. Serebriiskii and Lea Guo and Hironori Edamatsu and Hiroshi B. Koide and Sanjay T. Menon and Robert Eckl and Sukumar Sakamuri and Yingchun Lu and Quin-Zene Chen and Seema Agarwal and William R. Baumbach and Erica A Golemis and Fuyuhiko Tamanoi and Vladimir Khazak},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2002},
  volume={99 22},
  pages={
          14398-403
        }
}
The interaction of activated Ras with Raf initiates signaling cascades that contribute to a significant percentage of human tumors, suggesting that agents that specifically disrupt this interaction might have desirable chemotherapeutic properties. We used a subtractive forward two-hybrid approach to identify small molecule compounds that block the interaction of Ras with Raf. These compounds (MCP1 and its derivatives, 53 and 110) reduced serum-induced transcriptional activation of serum… CONTINUE READING

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