Tag: MEK

APS-2-79 is a KSR-Dependent Antagonist of RAF-Mediated MEK Phosphorylation

Deregulation of the Ras-MAPK pathway is an early event in many different cancers and a key driver of resistance to targeted therapies. Kinase suppressor of Ras (KSR) is a MAPK scaffold. KSR exhibits allosteric regulation through dimerization with RAF. In this study, researchers developed a class of compounds that...

MS432 is a Highly Selective PROTAC Degrader for MEK1 and MEK2

Chemical induced protein knockdown via the proteolysis targeting chimera (PROTAC) technology is a promising approach to target dysregulated proteins. Moreover, MEK1/2 proteins are the only RAF substrates. MEK1/2 proteins are the crucial “gatekeepers” of ERK activity. The classic RAS-RAF-MEK-ERK signaling pathway is common in mammals, plays critical roles in...