Raf

Raf

Function of Raf family kinases has been shown to play a role during organism development, cell cycle regulation, cell proliferation and differentiation, cell survival and apoptosis and many other cellular and physiological processes.

The RAF family of serine/threonine kinases are MAP3Ks that function downstream of the (PKA), and their inhibitory effects on CRAF activation can be overcome following dephosphorylation by PP2A. Other phosphorylation events are activating and occur following RAS-mediated recruitment to the plasma membrane. The phosphorylation of two residues within the N-region located at the amino terminus of CR3, Ser338 and Tyr341, is required for full activation of CRAF. The resultant negative charge in this region alleviates the intramolecular inhibition of the kinase domain by the N-terminus. While Src and Srcfamily kinases mediate the phosphorylation of Try341, the identity of the Ser338 kinase (or kinases) remains unclear. The p21 activated kinases (PAKs) have been implicated based on in vitro data, however, they fail to induce CRAF activation in a growth-factor dependent process. Two additional sites located within the kinase domain, Thr491 and Ser492, are essential for CRAF activation, however, the kinases that mediated their phosphorylation remain unknown; it is possible that these sites are subject to an auto-phosphorylating mechanism.

Reference:Eric Joseph. SMALL MOLECULE INHIBITION OF ACTIVATED MAP KINASE SIGNALING IN HUMAN CANCERS: BIOLOGICAL AND THERAPEUTIC IMPLICATIONS

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