Covalent inhibitors of KRASG12C have shown antitumor activity against
advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and …

Despite decades of research, efforts to directly target KRAS have been challenging.
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that …

KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the
treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of …

Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from
clinical studies of covalent KRASG12C inhibitors. Thus, inhibitors with broad potential for …

KRASG12C has emerged as a promising target in the treatment of solid tumors. Covalent
inhibitors targeting the mutant cysteine-12 residue have been shown to disrupt signaling by …

KRas is the most frequently mutated oncogene in human cancer, and even 40 years after
the initial discovery of Ras oncogenes in 1982, no approved drug directly targets Ras in Ras …

Recent progress in targeting KRASG12C has provided both insight and inspiration for
targeting alternative KRAS mutants. In this study, we evaluated the mechanism of action and …

The RAS oncogene is both the most frequently mutated oncogene in human cancer and the
first confirmed human oncogene to be discovered in 1982. After decades of research, in …

Capping off an era marred by drug development failures and punctuated by waning interest
and presumed intractability toward direct targeting of KRAS, new technologies and …

Summary KRAS G12C was recently identified to be potentially druggable by allele-specific
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …