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'Undruggable' mutation meets its match
Date:11/20/2013

In the field of drug design, the protein K-Ras is legendary. It's been on everyone's "target" list for more than 30 years due to its status as the most commonly mutated oncogene in human cancers. Despite this high profile, K-Ras has earned a reputation in scientific circles as being "undruggable" because many pharmaceutical, biotech, and academic laboratories have failed to design a drug that successfully targets the mutant gene.

Now, Howard Hughes Medical Institute (HHMI) researchers at the University of California, San Francisco have identified and exploited a newfound "Achilles heel" in K-Ras. The weak point is a newly discovered "pocket," or binding site, identified by HHMI investigator Kevan M. Shokat and colleagues. Shokat and his team have designed a chemical compound that fits inside this pocket and inhibits the normal activity of mutant K-Ras, but leaves the normal protein untouched.

"K-Ras is considered to be the most important oncogene in cancer and is widely believed to be 'undruggable,'" said Shokat. "We report the discovery of a new pocket on K-Ras that is druggable. We believe this has real translational implications for patients."

In a research article published November 20, 2013, in the journal Nature, Shokat's team describes a novel chemical compound that fits into a previously unknown pocket in K-Ras and interferes with function of the enzyme. The Ras proteins are small GTPase enzymes that transmit signals within cells. They are critical to cells because of the central role they play in cell growth and survival.

The name Ras also refers to the family of genes encoding those proteins. One of those genes, K-Ras, which was discovered nearly 30 years ago, is mutated in 30 percent of human tumors, including 90 percent of pancreatic cancers, 40 percent of colon cancers, and 20 percent of non-small cell lung cancers. Cancers with Ras mutations are aggressive and respond poorly to standard therapies.

Despite setbacks in t
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Contact: Jim Keeley
keeleyj@hhmi.org
301-215-8858
Howard Hughes Medical Institute
Source:Eurekalert

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