KRAS is an important protein in the RAS/MAPK signaling pathway. As a GTPase, KRAS converts GTP to GDP. Through GTP binding to KRAS, the protein is activated. The activation of KRAS sends off a chain reaction of activating downstream proteins, which then propagate growth factors and other cell signaling receptors. GTP/GDP functions as a molecular on/off switch for KRAS, where once KRAS converts GTP to GDP, KRAS is inactivated.
KRAS has always been regarded as a "Undruggable" targets because it doesn't have good druggable pocket and shows pM GTP affinity. May 28, 2021, the Food and Drug Administration (FDA) granted accelerated approval to the first KRAS G12C-blocking drug, called sotorasib. It’s a big breakthrough in the whole field forKRAS target. ICE scientist can supply the following assay test: