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Discovery of RAF Activation Mechanism May Aid Cancer Drug Development

A research team has shown that dimerization is essential for activation of the RAF protein kinase. When mutated, RAF protein kinase is responsible for more than 25 percent of human cancers. The research team believes that, by targeting the key dimerization process (specifically, the side-to-side dimerization of the kinase domain), it may be possible to develop new, more effective cancer therapies. "Protein kinases are the targets for some of the most successful anti-cancer drugs in the clinic," said Dr. Frank Sicheri, an author of the report. "Now that we have discovered how to turn off the RAF protein without interfering with other proteins, we may be able to design drugs that have unprecedented precision in targeting cancer cells while reducing the toxic side effects for patients." This work was published online in Nature on September 2. [Press release] [Nature abstract]