RAF proto-oncogene serine/threonine-protein kinase
Also known as: RAF, RAF1
Function
Serine/threonine-protein kinase that acts as a regulatory link between the membrane-associated Ras GTPases and the MAPK/ERK cascade, and this critical regulatory link functions as a switch determining cell fate decisions including proliferation, differentiation, apoptosis, survival and oncogenic transformation. RAF1 activation initiates a mitogen-activated protein kinase (MAPK) cascade that comprises a sequential phosphorylation of the dual-specific MAPK kinases (MAP2K1/MEK1 and MAP2K2/MEK2) and the extracellular signal-regulated kinases (MAPK3/ERK1 and MAPK1/ERK2). The phosphorylated form of RAF1 (on residues Ser-338 and Ser-339, by PAK1) phosphorylates BAD/Bcl2-antagonist of cell death at 'Ser-75'. Phosphorylates adenylyl cyclases: ADCY2, ADCY5 and ADCY6, resulting in their activation. Phosphorylates PPP1R12A resulting in inhibition of the phosphatase activity. Phosphorylates TNNT2/cardiac muscle troponin T. Can promote NF-kB activation and inhibit signal transducers involved in motility (ROCK2), apoptosis (MAP3K5/ASK1 and STK3/MST2), proliferation and angiogenesis (RB1). Can protect cells from apoptosis also by translocating to the mitochondria where it binds BCL2 and displaces BAD/Bcl2-antagonist of cell death. Regulates Rho signaling and migration, and is required for normal wound healing. Plays a role in the oncogenic transformation of epithelial cells via repression of the TJ protein, occludin (OCLN) by inducing the up-regulation of a transcriptional repressor SNAI2/SLUG, which induces down-regulation of OCLN. Restricts caspase activation in response to selected stimuli, notably Fas stimulation, pathogen-mediated macrophage apoptosis, and erythroid differentiation.
Classification
- Family (Pfam)
- PF00130 C1_1, PF07714 PK_Tyr_Ser-Thr, PF02196 RBD
- InterPro
- C1-like_sf, DAG/PE-bd, Kinase-like_dom_sf, PKC_DAG/PE, Prot_kinase_dom, Protein_kinase_ATP_BS, RBD_dom, Ser-Thr/Tyr_kinase_cat_dom, Ser/Thr_kinase_AS, Ser/Thr_Kinases-Pseudokinases, Ubiquitin-like_domsf
- Functional cluster
- Protein Serine/Threonine Kinases
Experimental structures · PDB · 67
- 1C1Y X-ray 1.90A
- 1FAQ NMR
- 1FAR NMR
- 1GUA X-ray 2.00A
- 1RFA NMR
- 3CU8 X-ray 2.40A
- 3IQJ X-ray 1.15A
- 3IQU X-ray 1.05A
- 3IQV X-ray 1.20A
- 3KUC X-ray 1.92A
- 3KUD X-ray 2.15A
- 3NKX X-ray 2.40A
- … and 55 more
A predicted model is available from AlphaFold.
Gene Ontology · 37
- GO:0005737 cytoplasm
- GO:0005829 cytosol
- GO:0005794 Golgi apparatus
- GO:0005741 mitochondrial outer membrane
- GO:0005739 mitochondrion
- GO:0005634 nucleus
- GO:0005886 plasma membrane
- GO:0031143 pseudopodium
- GO:0010856 adenylate cyclase activator activity
- GO:0005524 ATP binding
- GO:0019899 enzyme binding
- GO:0042802 identical protein binding
- GO:0004709 MAP kinase kinase kinase activity
- GO:0004672 protein kinase activity
- GO:0106310 protein serine kinase activity
- GO:0004674 protein serine/threonine kinase activity
- GO:0008270 zinc ion binding
- GO:0006915 apoptotic process
- GO:0038133 ERBB2-ERBB3 signaling pathway
- GO:0008286 insulin receptor signaling pathway
- GO:0048009 insulin-like growth factor receptor signaling pathway
- GO:0000165 MAPK cascade
- GO:0042552 myelination
- GO:0043066 negative regulation of apoptotic process
- GO:0008285 negative regulation of cell population proliferation
- GO:0031333 negative regulation of protein-containing complex assembly
- GO:0007528 neuromuscular junction development
- GO:0043410 positive regulation of MAPK cascade
- GO:0033138 positive regulation of peptidyl-serine phosphorylation
- GO:0006468 protein phosphorylation
- GO:0042981 regulation of apoptotic process
- GO:0045595 regulation of cell differentiation
- GO:0035023 regulation of Rho protein signal transduction
- GO:0014044 Schwann cell development
- GO:0007165 signal transduction
- GO:0060333 type II interferon-mediated signaling pathway
- GO:0042060 wound healing
Disease associations
- Noonan syndrome 5 MONDO:0012690
- LEOPARD syndrome 2 MONDO:0012691
- dilated cardiomyopathy 1NN MONDO:0014396
Drugs targeting this protein · 8
- SORAFENIB TOSYLATE inhibitor
- REGORAFENIB inhibitor
- TOVORAFENIB inhibitor
- XL-281 inhibitor
- LY-3009120 inhibitor
- BELVARAFENIB inhibitor
- NAPORAFENIB inhibitor
- ARQ-736 inhibitor
Related proteins · sequence + function similarity
- RAF proto-oncogene serine/threonine-protein kinase 1.00
- RAF proto-oncogene serine/threonine-protein kinase 1.00
- RAF proto-oncogene serine/threonine-protein kinase 1.00
- RAF proto-oncogene serine/threonine-protein kinase 1.00
- RAF proto-oncogene serine/threonine-protein kinase 0.99
- RAF proto-oncogene serine/threonine-protein kinase 0.98
- Raf homolog serine/threonine-protein kinase Raf 0.91
- Serine/threonine-protein kinase A-Raf 0.90
- Serine/threonine-protein kinase A-Raf 0.90
- Serine/threonine-protein kinase A-Raf 0.89
- Serine/threonine-protein kinase A-Raf 0.89
- Serine/threonine-protein kinase B-raf 0.89
Co-cited proteins · studied together in the literature
- Calcipressin-1 1 shared papers
- Zinc finger protein SNAI2 1 shared papers
- RAF proto-oncogene serine/threonine-protein kinase 2 shared papers
- Ras-related protein Rap-1A 2 shared papers
- Protein FAM83B 1 shared papers
- RAF proto-oncogene serine/threonine-protein kinase 1 shared papers
- Serine/threonine-protein kinase PAK 5 1 shared papers
- Phosphatidylethanolamine-binding protein 1 1 shared papers
- Leucine-rich repeat protein SHOC-2 5 shared papers
- Malignant fibrous histiocytoma-amplified sequence 1 1 shared papers
- Diacylglycerol kinase eta 1 shared papers
- Son of sevenless homolog 1 1 shared papers
Literature · 67 cited papers
- Structure-function analysis of the SHOC2-MRAS-PP1c holophosphatase complex. Nature · 2022
- Structure of the MRAS-SHOC2-PP1C phosphatase complex. Nature · 2022
- Structural basis for SHOC2 modulation of RAS signalling. Nature · 2022
- A YWHAZ variant associated with cardiofaciocutaneous syndrome activates the RAF-ERK pathway. Front. Physiol. · 2019
- Delineation of LZTR1 mutation-positive patients with Noonan syndrome and identification of LZTR1 binding to RAF1-PPP1CB complexes. Hum. Genet. · 2019
- Tumor suppressor Tsc1 is a new Hsp90 co-chaperone that facilitates folding of kinase and non-kinase clients. EMBO J. · 2017
- RAF1 mutations in childhood-onset dilated cardiomyopathy. Nat. Genet. · 2014
- An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. J. Proteomics · 2014
- Phosphodiesterase-8A binds to and regulates Raf-1 kinase. Proc. Natl. Acad. Sci. U.S.A. · 2013
- MASL1 induces erythroid differentiation in human erythropoietin-dependent CD34+ cells through the Raf/MEK/ERK pathway. Blood · 2013
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- FAM83B mediates EGFR- and RAS-driven oncogenic transformation. J. Clin. Invest. · 2012
- … and 55 more in the literature graph