Tag Archives: shokat

Drug strategy blocks leading driver of cancer

Using a new strategy, UC San Francisco researchers have succeeded in making small molecules that irreversibly target a mutant form of this protein, called ras, without binding to the normal form. This feature distinguishes the molecules from all other targeted drug treatments in cancer, according to the researchers. When tested on human lung cancer cells grown in culture, the molecules efficiently killed the ras-driven cancer cells. …

‘Undruggable’ mutation meets its match

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…