Article
BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition.
Cancer discovery - 1 Jan 2021
Hofmann Marco H, Gmachl Michael, Ramharter Juergen, Savarese Fabio, Gerlach Daniel, Marszalek Joseph R, Sanderson Michael P, Kessler Dirk, Trapani Francesca, Arnhof Heribert, Rumpel Klaus, Botesteanu Dana-Adriana, Ettmayer Peter, Gerstberger Thomas, Kofink Christiane, Wunberg Tobias, Zoephel Andreas, Fu Szu-Chin, Teh Jessica L, Böttcher Jark, Pototschnig Nikolai, Schachinger Franziska, Schipany Katharina, Lieb Simone, Vellano Christopher P, O'Connell Jonathan C, Mendes Rachel L, Moll Jurgen, Petronczki Mark, Heffernan Timothy P, Pearson Mark, McConnell Darryl B, Kraut Norbert
Abstract excerpt
KRAS is the most frequently mutated driver of pancreatic, colorectal, and non-small cell lung cancers. Direct KRAS blockade has proved challenging, and inhibition of a key downstream effector pathway, the RAF-MEK-ERK cascade, has shown limited success because of activation of feedback networks that keep the pathway in check. We hypothesized that inhibiting SOS1, a KRAS activator and important feedback node,...
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