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First-of-its-kind study creates new tool for targeted cancer drug development
Date:10/30/2011

ent kinases performing numerous functions. And the vast majority of kinase inhibitors will act on more than one kinase, and so have the potential to interfere with both cancer and the normal processes the body needs for health and survival. Not surprisingly, some of the kinase inhibitors approved for use in cancer cause significant side effects, such as cardiovascular problems.

Until the last few years, however, researchers simply didn't have the technology to observe which kinases a specific inhibitor acted upon. Recently, however, the company Reaction Biology Corporation developed a way to observe the suite of effects from one kinase inhibitor.

For the first time, Peterson and his team catalogued the activity of 178 kinase inhibitors against 300 kinases. The experiment was like observing what happens after shooting a scattergun at a wall of balloons, he says. Before, scientists could only tell if you popped one particular balloon now, however, they can see if other balloons were hit, as well. "We're essentially shining a light on the wall of balloons so we have a much better view of the balloons that were popped."

Not surprisingly, the researchers found that kinase inhibitors targeted multiple kinases, even some that appeared to be unrelated to each other. They have deposited this massive library of results on a free website so scientists studying kinases and inhibitors can learn more about their multiple interactions.

The fact that kinase inhibitors target multiple kinases may actually be a good thing, says Peterson. Initially, scientists had hoped to find an inhibitor that targets one specific kinase involved in cancer; now, they realize that cancer rarely results from one kinase. Instead, multiple kinases likely collaborate to produce the disease -- so to stop that process, you may have to hit all of those kinases together. "It may not be possible to develop a successful drug against one kinase," he says. Indeed, some kinase
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Contact: Diana Quattrone
Diana.Quattrone@fccc.edu
215-728-7784
Fox Chase Cancer Center
Source:Eurekalert

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