Focal adhesion kinase 1
Also known as: FAK, FAK1, PTK2
Function
Non-receptor protein-tyrosine kinase that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adhesions and cell protrusions, cell cycle progression, cell proliferation and apoptosis. Required for early embryonic development and placenta development. Required for embryonic angiogenesis, normal cardiomyocyte migration and proliferation, and normal heart development. Regulates axon growth and neuronal cell migration, axon branching and synapse formation; required for normal development of the nervous system. Plays a role in osteogenesis and differentiation of osteoblasts. Functions in integrin signal transduction, but also in signaling downstream of numerous growth factor receptors, G protein-coupled receptors (GPCR), EPHA2, netrin receptors and LDL receptors. Forms multisubunit signaling complexes with SRC and SRC family members upon activation; this leads to the phosphorylation of additional tyrosine residues, creating binding sites for scaffold proteins, effectors and substrates. Regulates numerous signaling pathways. Promotes activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascade. Promotes activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling cascade. Promotes localized and transient activation of guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs), and thereby modulates the activity of Rho family GTPases. Signaling via CAS family members mediates activation of RAC1. Phosphorylates NEDD9 following integrin stimulation. Recruits the ubiquitin ligase MDM2 to P53/TP53 in the nucleus, and thereby regulates P53/TP53 activity, P53/TP53 ubiquitination and proteasomal degradation. Phosphorylates SRC; this increases SRC kinase activity. Phosphorylates ACTN1, ARHGEF7, GRB7, RET and WASL. Promotes phosphorylation of PXN and STAT1; most likely PXN and STAT1 are phosphorylated by a SRC family kinase that is recruited to autophosphorylated PTK2/FAK1, rather than by PTK2/FAK1 itself. Promotes phosphorylation of BCAR1; GIT2 and SHC1; this requires both SRC and PTK2/FAK1. Promotes phosphorylation of BMX and PIK3R1. Isoform 6 (FRNK) does not contain a kinase domain and inhibits PTK2/FAK1 phosphorylation and signaling. Its enhanced expression can attenuate the nuclear accumulation of LPXN and limit its ability to enhance serum response factor (SRF)-dependent gene transcription.
Classification
- Family (Pfam)
- PF21477 FERM_C_FAK1, PF00373 FERM_M, PF18038 FERM_N_2, PF03623 Focal_AT, PF07714 PK_Tyr_Ser-Thr
- InterPro
- Band_41_domain, FADK_N, FAK1-like_FERM_C, FAK1/PYK2_FERM_C, FERM/acyl-CoA-bd_prot_sf, FERM_2, FERM_central, FERM_domain, Focal_adhe_kin_target_dom_sf, Focal_adhesion_kin_target_dom, Kinase-like_dom_sf, PH-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, Ser-Thr/Tyr_kinase_cat_dom, Tyr_kinase_AS, Tyr_kinase_cat_dom, Ubiquitin-like_domsf
- Functional cluster
- Protein Serine/Threonine Kinases
Experimental structures · PDB · 40
- 1K04 X-ray 1.95A
- 1K05 X-ray 2.90A
- 1MP8 X-ray 1.60A
- 1OW6 X-ray 2.35A
- 1OW7 X-ray 2.60A
- 1OW8 X-ray 2.85A
- 2ETM X-ray 2.30A
- 2IJM X-ray 2.19A
- 3B71 X-ray 2.82A
- 3BZ3 X-ray 2.20A
- 3PXK X-ray 1.79A
- 3S9O X-ray 2.60A
- … and 28 more
A predicted model is available from AlphaFold.
Gene Ontology · 63
- GO:0005938 cell cortex
- GO:0005813 centrosome
- GO:0036064 ciliary basal body
- GO:0005856 cytoskeleton
- GO:0005829 cytosol
- GO:0005925 focal adhesion
- GO:0005634 nucleus
- GO:0048471 perinuclear region of cytoplasm
- GO:0005886 plasma membrane
- GO:0001725 stress fiber
- GO:0003779 actin binding
- GO:0005524 ATP binding
- GO:0005178 integrin binding
- GO:0008432 JUN kinase binding
- GO:0140677 molecular function activator activity
- GO:0004715 non-membrane spanning protein tyrosine kinase activity
- GO:0019901 protein kinase binding
- GO:0019903 protein phosphatase binding
- GO:0004713 protein tyrosine kinase activity
- GO:0004725 protein tyrosine phosphatase activity
- GO:0042169 SH2 domain binding
- GO:0001525 angiogenesis
- GO:0007411 axon guidance
- GO:0016477 cell migration
- GO:0048870 cell motility
- GO:0035995 detection of muscle stretch
- GO:0048013 ephrin receptor signaling pathway
- GO:0007173 epidermal growth factor receptor signaling pathway
- GO:0030010 establishment of cell polarity
- GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis
- GO:0060396 growth hormone receptor signaling pathway
- GO:0003007 heart morphogenesis
- GO:0007229 integrin-mediated signaling pathway
- GO:2000811 negative regulation of anoikis
- GO:0043066 negative regulation of apoptotic process
- GO:0033629 negative regulation of cell adhesion mediated by integrin
- GO:0022408 negative regulation of cell-cell adhesion
- GO:0038007 netrin-activated signaling pathway
- GO:0001890 placenta development
- GO:0030335 positive regulation of cell migration
- GO:0008284 positive regulation of cell population proliferation
- GO:0033634 positive regulation of cell-cell adhesion mediated by integrin
- GO:0010634 positive regulation of epithelial cell migration
- GO:0010718 positive regulation of epithelial to mesenchymal transition
- GO:0010763 positive regulation of fibroblast migration
- GO:0010759 positive regulation of macrophage chemotaxis
- GO:0120041 positive regulation of macrophage proliferation
- GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- GO:2000060 positive regulation of ubiquitin-dependent protein catabolic process
- GO:0090303 positive regulation of wound healing
- GO:0030155 regulation of cell adhesion
- GO:0042127 regulation of cell population proliferation
- GO:0008360 regulation of cell shape
- GO:0051493 regulation of cytoskeleton organization
- GO:0010594 regulation of endothelial cell migration
- GO:0010632 regulation of epithelial cell migration
- GO:0051893 regulation of focal adhesion assembly
- GO:0045667 regulation of osteoblast differentiation
- GO:1900024 regulation of substrate adhesion-dependent cell spreading
- GO:0007172 signal complex assembly
- GO:0007179 transforming growth factor beta receptor signaling pathway
- GO:0097706 vascular endothelial cell response to oscillatory fluid shear stress
- GO:0048010 vascular endothelial growth factor receptor signaling pathway
Drugs targeting this protein · 7
- PF-00562271 inhibitor
- VS-4718 inhibitor
- DEFACTINIB inhibitor
- IFEBEMTINIB inhibitor
- CONTELTINIB inhibitor
- CEP-37440 inhibitor
- GSK-2256098 inhibitor
Neighborhood · nearest proteins
Related proteins · sequence + function similarity
- Focal adhesion kinase 1 1.00
- Focal adhesion kinase 1 1.00
- Focal adhesion kinase 1 0.99
- Focal adhesion kinase 1 0.98
- Protein-tyrosine kinase 2-beta 0.83
- Protein-tyrosine kinase 2-beta 0.83
- Protein-tyrosine kinase 2-beta 0.82
- Serine/threonine-protein kinase B-raf 0.76
- Serine/threonine-protein kinase B-raf 0.75
- RAF proto-oncogene serine/threonine-protein kinase 0.75
- Inactive tyrosine-protein kinase kin-32 0.74
- RAF proto-oncogene serine/threonine-protein kinase 0.74
Co-cited proteins · studied together in the literature
- Forkhead box protein J1 1 shared papers
- Cas scaffolding protein family member 4 1 shared papers
- Focal adhesion kinase 1 7 shared papers
- Leupaxin 2 shared papers
- Zinc finger FYVE domain-containing protein 21 1 shared papers
- Zinc finger FYVE domain-containing protein 21 1 shared papers
- Metalloreductase STEAP4 1 shared papers
- Protein-tyrosine kinase 2-beta 3 shared papers
- Cytoplasmic tyrosine-protein kinase BMX 2 shared papers
- Epithelial membrane protein 2 1 shared papers
- Tyrosine-protein kinase Fer 2 shared papers
- T-cell surface glycoprotein CD4 1 shared papers
Literature · 73 cited papers
- De Novo Mutations in FOXJ1 Result in a Motile Ciliopathy with Hydrocephalus and Randomization of Left/Right Body Asymmetry. Am. J. Hum. Genet. · 2019
- The Intracranial Aneurysm Gene THSD1 Connects Endosome Dynamics to Nascent Focal Adhesion Assembly. Cell. Physiol. Biochem. · 2017
- MISP is a novel Plk1 substrate required for proper spindle orientation and mitotic progression. J. Cell Biol. · 2013
- A novel splice variant of calcium and integrin-binding protein 1 mediates protein kinase D2-stimulated tumour growth by regulating angiogenesis. Oncogene · 2014
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- Focal adhesion kinase: exploring Fak structure to gain insight into function. Int. Rev. Cell Mol. Biol. · 2011
- Focal adhesion kinase (FAK) binds RET kinase via its FERM domain, priming a direct and reciprocal RET-FAK transactivation mechanism. J. Biol. Chem. · 2011
- Initial characterization of the human central proteome. BMC Syst. Biol. · 2011
- Comprehensive analysis of phosphorylation sites in Tensin1 reveals regulation by p38MAPK. Mol. Cell. Proteomics · 2010
- The role of focal adhesion kinase in early development. Histol. Histopathol. · 2010
- Focal adhesion kinase and p53 signal transduction pathways in cancer. Front. Biosci. · 2010
- Bioluminescent imaging study: FAK inhibitor, PF-562,271, preclinical study in PC3M-luc-C6 local implant and metastasis xenograft models. Cancer Biol. Ther. · 2010
- … and 61 more in the literature graph