Although several covalent KRAS G12C inhibitors have made great progress in the treatment
of KRAS G12C-mutant cancer, their clinical applications are limited by adaptive resistance …

KRASG12D, the most frequent KRAS oncogenic mutation, is a promising target for cancer
therapy. Herein, we report the design, synthesis, and biological evaluation of a series of …

KRAS is mutated in∼ 20% of human cancers and is one of the most sought-after targets for
pharmacological modulation, despite having historically been considered “undruggable.” …

KRAS is the most frequently mutated oncogene found in pancreatic, colorectal, and lung
cancers. Although it has been challenging to identify targeted therapies for cancers …

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

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 …

Abstract A series of KRAS G12C-targeting PROTACs (PROteolysis TArgeting Chimeras)
were designed and synthesized based on KRas G12C-IN-3 (a KRAS G12C inhibitor) and …

KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the
treatment of pancreatic cancer. Herein, we identified four potent and noncovalent …

Background: KRAS is one of the most frequently mutated oncogenes in various cancers.
Among KRAS mutations, KRAS G12D is the most frequent driver mutation and is found in …

Summary KRAS G12D is the most frequently mutated oncogenic KRAS subtype in solid
tumors and remains undruggable in clinical settings. Here, we developed a high affinity …