Tag: KRAS G12C

AMG-510 is a First-in-Class, Orally Active, and Selective KRAS G12C Inhibitor

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. They are involved in tumor cell growth and survival. Somatic, activating mutations in KRAS are a hallmark of cancer. Furthermore, they prevent the association of GTPase-activating proteins, thus stabilizing effector binding and enhancing KRAS signaling....

MRTX849 is an Orally Active and Covalent Inhibitor of KRAS G12C

KRAS mutations are the most common mutations. Especially, the KRAS oncogene encodes a binding protein that plays a crucial role in transmitting signals from extracellular growth factors to the cell nucleus. KRAS mutations occur commonly in colorectal carcinomas. KRASG12C mutations are present in lung and colon adenocarcinoma as well...

ARS-1620, a G12C-Specific Inhibitor, is a Promising Candidate for KRAS-mutant Cancer

KRAS mutations have wide-spread prevalence in human cancers nowadays. The mis-sense mutation of KRAS at codon 12 aberrantly activates the protein into a hyperexcitable state. Attenuating its GTPase activity results in accretion of GTP-bound activated KRAS and activation of downstream signaling pathways. Ideally, the KRASG12C protein product is an...

ARS-853 is a Selective KRAS (G12C) Inhibitor

KRAS mutations have wide-spread prevalence in human cancers nowadays. KRASG12C mutations occur in 16% of lung adenocarcinomas, making them one of the most frequent activating genetic alterations in lung cancer. The mis-sense mutation of KRAS at codon 12 aberrantly activates the protein into a hyperexcitable state. Attenuating its GTPase...