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The Raf kinase inhibitor protein (RKIP) is a kinase inhibitor protein, that regulates many signaling pathways within the cell. [1] RKIP is a member of the phosphatidylethanolamine-binding protein family and has displayed disruptive regulation on the Raf-1-MEK1/2, ERK1/2 and NF-kappaB signalling pathways, by interaction with the Raf-1 kinase.
RAF is an acronym for Rapidly Accelerated Fibrosarcoma. [12] RAF kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade. [11] Activation of RAF kinases requires interaction with RAS-GTPases. The three RAF kinase family members are: A-RAF; B-RAF; c-Raf
The first drug licensed to act on this pathway is sorafenib — a Raf kinase inhibitor. Other Raf inhibitors include SB590885, PLX4720, XL281, RAF265, encorafenib, dabrafenib, and vemurafenib. [18] Some MEK inhibitors include cobimetinib, CI-1040, PD0325901, binimetinib (MEK162), selumetinib, [18] and trametinib (GSK1120212) [20]
B-Raf is a 766-amino acid, regulated signal transduction serine/threonine-specific protein kinase.Broadly speaking, it is composed of three conserved domains characteristic of the Raf kinase family: conserved region 1 (CR1), a Ras-GTP-binding [11] self-regulatory domain, conserved region 2 (CR2), a serine-rich hinge region, and conserved region 3 (CR3), a catalytic protein kinase domain that ...
RAF proto-oncogene serine/threonine-protein kinase, also known as proto-oncogene c-RAF or simply c-Raf or even Raf-1, is an enzyme [4] that in humans is encoded by the RAF1 gene. [ 5 ] [ 6 ] The c-Raf protein is part of the ERK1/2 pathway as a MAP kinase (MAP3K) that functions downstream of the Ras subfamily of membrane associated GTPases. [ 7 ]
Flezurafenib is an investigational new drug designed as a rapidly accelerated fibrosarcoma (RAF) kinase inhibitor which is being evaluated for the treatment of cancer. . Developed by Jazz Pharmaceuticals, this novel therapeutic agent is currently being explored for its efficacy against solid tumors and hematological malignancies harboring oncogenic mutations that activate the RAS-RAF-MAPK ...
Encorafenib acts as an ATP-competitive RAF kinase inhibitor, decreasing ERK phosphorylation and down-regulation of CyclinD1. [10] This arrests the cell cycle in G1 phase, inducing senescence without apoptosis. [10] Therefore, it is only effective in melanomas with a BRAF mutation, which make up 50% of all melanomas. [11]
For example, KSR1 and KSR2 are actually MAP3 kinases and related to the Raf proteins. [37] Although KSRs alone display negligible MAP3 kinase activity, KSR proteins can still participate in the activation of Raf kinases by forming side-to-side heterodimers with them, providing an allosteric pair to turn on each enzymes. [38]