Suppressing Nucleotide Exchange to Inhibit KRAS-Mutant Tumors.

ABSTRACT

Guanine nucleotide exchange factors (GEF) control the rate-limiting step of physiologic RAS activation. In this issue of Cancer Discovery, Hofmann and colleagues describe the discovery of a selective inhibitor targeting the GEF, SOS1, along with its preclinical effects in suppressing KRAS-mutant tumor growth.See related article by Hofmann et al., p. 142.