Tag: RAF

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...

Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor

ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...

ML786 is an Orally Bioavailable Raf Inhibitor

The mitogen-activated protein kinase (MAPK) signal pathway plays an important role in cells. It also has a response to many different external stimuli and regulates cellular growth, proliferation. The Raf isoform B-Raf is one component of this pathway. Besides, it has a high rate of activating mutation in melanoma...

MCP110 is an Inhibitor of Ras/Raf-1 Interaction

Ras is a small GTPase and interacts with the protein Raf to create activated Ras-Raf complex that activates the downstream effectors in the ERK pathway. Malfunctioning Ras-Raf switches cause cancer. Ras-Raf interaction has taken a center stage in cancer research. Ras is a peripheral membrane protein that acts as...

BI-882370 is a Novel Orally Active RAF Kinase Inhibitor

Cancers arise owing to the accumulation of mutations in critical genes that alter normal programmes of cell proliferation, differentiation and death. The RAS–RAF–MEK–ERK–MAP kinase pathway mediates cellular responses to growth signals. Three RAF genes code for cytoplasmic serine/threonine kinases. Whereas mutations in ARAF and CRAF are very rare, BRAF...

A Novel and Efficacious RAF Inhibitor RAF709

The mitogen-activated protein kinase pathway regulates lots of multiple biological functions. In addition, RAF inhibitors activate the MAPK pathway. Interestingly, the MAPK pathway in turn induces the RAS proteins to exchange GDP for GTP. The RAF proteins are serine-threonine specific protein kinases. They activate the MEK/ERK cascade downstream of...