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.
30 year study of paramount cancer gene finally decoded for destruction
