Protein-tyrosine kinase 2-beta
Also known as: FAK2, PTK2B, PYK2, RAFTK
Function
Non-receptor protein-tyrosine kinase that regulates reorganization of the actin cytoskeleton, cell polarization, cell migration, adhesion, spreading and bone remodeling. Plays a role in the regulation of the humoral immune response, and is required for normal levels of marginal B-cells in the spleen and normal migration of splenic B-cells. Required for normal macrophage polarization and migration towards sites of inflammation. Regulates cytoskeleton rearrangement and cell spreading in T-cells, and contributes to the regulation of T-cell responses. Promotes osteoclastic bone resorption; this requires both PTK2B/PYK2 and SRC. May inhibit differentiation and activity of osteoprogenitor cells. Functions in signaling downstream of integrin and collagen receptors, immune receptors, G protein-coupled receptors (GPCR), cytokine, chemokine and growth factor receptors, and mediates responses to cellular stress. 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 of the AKT1 signaling cascade. Promotes activation of NOS3. Regulates production of the cellular messenger cGMP. Promotes activation of the MAP kinase signaling cascade, including activation of MAPK1/ERK2, MAPK3/ERK1 and MAPK8/JNK1. Promotes activation of Rho family GTPases, such as RHOA and RAC1. Recruits the ubiquitin ligase MDM2 to P53/TP53 in the nucleus, and thereby regulates P53/TP53 activity, P53/TP53 ubiquitination and proteasomal degradation. Acts as a scaffold, binding to both PDPK1 and SRC, thereby allowing SRC to phosphorylate PDPK1 at 'Tyr-9, 'Tyr-373', and 'Tyr-376'. Promotes phosphorylation of NMDA receptors by SRC family members, and thereby contributes to the regulation of NMDA receptor ion channel activity and intracellular Ca(2+) levels. May also regulate potassium ion transport by phosphorylation of potassium channel subunits. Phosphorylates SRC; this increases SRC kinase activity. Phosphorylates ASAP1, NPHP1, KCNA2 and SHC1. Promotes phosphorylation of ASAP2, RHOU and PXN; this requires both SRC and PTK2/PYK2.
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
- Zinc-Finger & Chromatin Regulatory Proteins
Experimental structures · PDB · 26
- 2LK4 NMR
- 3CC6 X-ray 1.60A
- 3ET7 X-ray 2.70A
- 3FZO X-ray 2.20A
- 3FZP X-ray 2.10A
- 3FZR X-ray 2.70A
- 3FZS X-ray 1.75A
- 3FZT X-ray 1.95A
- 3GM1 X-ray 2.95A
- 3GM2 X-ray 2.71A
- 3GM3 X-ray 2.60A
- 3H3C X-ray 2.00A
- … and 14 more
A predicted model is available from AlphaFold.
Gene Ontology · 78
- GO:0097440 apical dendrite
- GO:0044297 cell body
- GO:0005938 cell cortex
- GO:0005737 cytoplasm
- GO:0005829 cytosol
- GO:0030425 dendrite
- GO:0005925 focal adhesion
- GO:0098978 glutamatergic synapse
- GO:0030426 growth cone
- GO:0030027 lamellipodium
- GO:0043025 neuronal cell body
- GO:0017146 NMDA selective glutamate receptor complex
- GO:0005634 nucleus
- GO:0048471 perinuclear region of cytoplasm
- GO:0005886 plasma membrane
- GO:0014069 postsynaptic density
- GO:0099092 postsynaptic density, intracellular component
- GO:0098793 presynapse
- GO:0005524 ATP binding
- GO:0004683 calcium/calmodulin-dependent protein kinase activity
- GO:0035255 ionotropic glutamate receptor binding
- GO:0099602 neurotransmitter receptor regulator activity
- GO:0004715 non-membrane spanning protein tyrosine kinase activity
- GO:0004713 protein tyrosine kinase activity
- GO:0030546 signaling receptor activator activity
- GO:0042976 activation of Janus kinase activity
- GO:0002250 adaptive immune response
- GO:0006915 apoptotic process
- GO:0045453 bone resorption
- GO:0007166 cell surface receptor signaling pathway
- GO:0006968 cellular defense response
- GO:0071300 cellular response to retinoic acid
- GO:0070098 chemokine-mediated signaling pathway
- GO:0030865 cortical cytoskeleton organization
- GO:0086100 endothelin receptor signaling pathway
- GO:0007173 epidermal growth factor receptor signaling pathway
- GO:0007229 integrin-mediated signaling pathway
- GO:0035235 ionotropic glutamate receptor signaling pathway
- GO:0060291 long-term synaptic potentiation
- GO:0002315 marginal zone B cell differentiation
- GO:0043066 negative regulation of apoptotic process
- GO:0030502 negative regulation of bone mineralization
- GO:0008285 negative regulation of cell population proliferation
- GO:0045638 negative regulation of myeloid cell differentiation
- GO:0043524 negative regulation of neuron apoptotic process
- GO:0043267 negative regulation of potassium ion transport
- GO:0038083 peptidyl-tyrosine autophosphorylation
- GO:0018108 peptidyl-tyrosine phosphorylation
- GO:0030838 positive regulation of actin filament polymerization
- GO:0045766 positive regulation of angiogenesis
- GO:2000538 positive regulation of B cell chemotaxis
- GO:0030335 positive regulation of cell migration
- GO:0008284 positive regulation of cell population proliferation
- GO:0001954 positive regulation of cell-matrix adhesion
- GO:0010595 positive regulation of endothelial cell migration
- GO:0070374 positive regulation of ERK1 and ERK2 cascade
- GO:2000463 positive regulation of excitatory postsynaptic potential
- GO:0046330 positive regulation of JNK cascade
- GO:0010976 positive regulation of neuron projection development
- GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- GO:0045860 positive regulation of protein kinase activity
- GO:0051968 positive regulation of synaptic transmission, glutamatergic
- GO:2000060 positive regulation of ubiquitin-dependent protein catabolic process
- GO:0046777 protein autophosphorylation
- GO:0065003 protein-containing complex assembly
- GO:0032956 regulation of actin cytoskeleton organization
- GO:0030155 regulation of cell adhesion
- GO:0008360 regulation of cell shape
- GO:0010758 regulation of macrophage chemotaxis
- GO:0099151 regulation of postsynaptic density assembly
- GO:0051279 regulation of release of sequestered calcium ion into cytosol
- GO:0048167 regulation of synaptic plasticity
- GO:2000058 regulation of ubiquitin-dependent protein catabolic process
- GO:0007172 signal complex assembly
- GO:0007165 signal transduction
- GO:0002040 sprouting angiogenesis
- GO:0033209 tumor necrosis factor-mediated signaling pathway
- GO:0048010 vascular endothelial growth factor receptor signaling pathway
Drugs targeting this protein · 2
- DEFACTINIB inhibitor
- CONTELTINIB inhibitor
Related proteins · sequence + function similarity
- Protein-tyrosine kinase 2-beta 1.00
- Protein-tyrosine kinase 2-beta 1.00
- Focal adhesion kinase 1 0.83
- Focal adhesion kinase 1 0.82
- Focal adhesion kinase 1 0.82
- Focal adhesion kinase 1 0.82
- Focal adhesion kinase 1 0.78
- Inactive tyrosine-protein kinase kin-32 0.78
- Tyrosine-protein kinase Fgr 0.73
- Tyrosine-protein kinase Blk 0.73
- Proto-oncogene tyrosine-protein kinase LCK 0.72
- Tyrosine-protein kinase Src-1 0.72
Co-cited proteins · studied together in the literature
- Protein-tyrosine kinase 2-beta 4 shared papers
- Protein-tyrosine kinase 2-beta 5 shared papers
- Arf-GAP with SH3 domain, ANK repeat and PH domain-containing protein 1 1 shared papers
- Rho-related GTP-binding protein RhoU 1 shared papers
- Focal adhesion kinase 1 3 shared papers
- Nephrocystin-1 1 shared papers
- RB1-inducible coiled-coil protein 1 1 shared papers
- Proto-oncogene vav 1 shared papers
- Ephrin type-A receptor 1 1 shared papers
- Paxillin 1 shared papers
- Tyrosine-protein phosphatase non-receptor type 12 1 shared papers
- Leupaxin 1 shared papers
Literature · 48 cited papers
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- Proline-rich tyrosine kinase 2 (Pyk2) promotes cell motility of hepatocellular carcinoma through induction of epithelial to mesenchymal transition. PLoS ONE · 2011
- Nephrocystin-4 regulates Pyk2-induced tyrosine phosphorylation of nephrocystin-1 to control targeting to monocilia. J. Biol. Chem. · 2011
- Initial characterization of the human central proteome. BMC Syst. Biol. · 2011
- Redox sensitive Pyk2 as a target for therapeutics in breast cancer. Front. Biosci. · 2011
- Recruitment of Pyk2 to SHPS-1 signaling complex is required for IGF-I-dependent mitogenic signaling in vascular smooth muscle cells. Cell. Mol. Life Sci. · 2010
- T cell receptor activation leads to two distinct phases of Pyk2 activation and actin cytoskeletal rearrangement in human T cells. Mol. Immunol. · 2010
- Cellular functions of FAK kinases: insight into molecular mechanisms and novel functions. J. Cell Sci. · 2010
- The T cell receptor-mediated phosphorylation of Pyk2 tyrosines 402 and 580 occurs via a distinct mechanism than other receptor systems. J. Leukoc. Biol. · 2010
- Targeting Pyk2 for therapeutic intervention. Expert Opin. Ther. Targets · 2010
- Pyk2 inhibition of p53 as an adaptive and intrinsic mechanism facilitating cell proliferation and survival. J. Biol. Chem. · 2010
- Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells. Bioorg. Med. Chem. Lett. · 2009
- … and 36 more in the literature graph