Tyrosine-protein kinase JAK2
Also known as: JAK2
Function
Non-membrane spanning protein tyrosine kinase that phosphorylates type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin receptor (MPL/TPOR); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Functionnally, plays a pivotal role in signal transduction and is involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. Mechanistically, following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B). In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin. Up-regulates the potassium voltage-gated channel activity of KCNA3. Binding of CNTF or the CLCF1/CLF heterodimer to CNTFR leads to IL6ST/gp130-LIFR dimerization followed by activation of JAK1 and JAK2 which in turns phosphorylate IL6ST/gp130 and LIFR. The tyrosine phosphorylated signaling receptors serve in turn as docking proteins for STAT3. Involved in the oncostatin-M-mediated signaling pathway through both type I OSM receptor complex (heterodimers composed of LIFR and IL6ST) and type II OSM receptor complex (heterodimers composed of OSMR and IL6ST).
Classification
- Family (Pfam)
- PF18379 FERM_F1, PF18377 FERM_F2, PF17887 Jak1_Phl, PF07714 PK_Tyr_Ser-Thr, PF21990 SH2_1
- InterPro
- Band_41_domain, FERM_2, FERM_central, FERM_domain, FERM_F1, FERM_F2, JAK, JAK1-3/TYK2_PHL_dom, JAK2_FERM_C-lobe, JAK2_SH2, Kinase-like_dom_sf, PH-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, PTK_Jak2_rpt1, PTKc_Jak2_rpt2, Ser-Thr/Tyr_kinase_cat_dom, SH2, SH2_dom_sf, Tyr_kinase_AS, Tyr_kinase_cat_dom, Tyr_kinase_non-rcpt_Jak/Tyk2, Tyr_kinase_non-rcpt_Jak2
- Functional cluster
- Serine/Threonine Protein Kinases
Experimental structures · PDB · 164
- 2B7A X-ray 2.00A
- 2W1I X-ray 2.60A
- 2XA4 X-ray 2.04A
- 3E62 X-ray 1.92A
- 3E63 X-ray 1.90A
- 3E64 X-ray 1.80A
- 3FUP X-ray 2.40A
- 3IO7 X-ray 2.60A
- 3IOK X-ray 2.10A
- 3JY9 X-ray 2.10A
- 3KCK X-ray 2.20A
- 3KRR X-ray 1.80A
- … and 152 more
A predicted model is available from AlphaFold.
Gene Ontology · 114
- GO:0005901 caveola
- GO:0000785 chromatin
- GO:0005737 cytoplasm
- GO:0009898 cytoplasmic side of plasma membrane
- GO:0005829 cytosol
- GO:0031904 endosome lumen
- GO:0000791 euchromatin
- GO:0031234 extrinsic component of cytoplasmic side of plasma membrane
- GO:0019897 extrinsic component of plasma membrane
- GO:0098978 glutamatergic synapse
- GO:0045121 membrane raft
- GO:0005654 nucleoplasm
- GO:0005634 nucleus
- GO:0005886 plasma membrane
- GO:0098794 postsynapse
- GO:0033130 acetylcholine receptor binding
- GO:0005524 ATP binding
- GO:0005131 growth hormone receptor binding
- GO:0020037 heme binding
- GO:0042393 histone binding
- GO:0035401 histone H3Y41 kinase activity
- GO:0042802 identical protein binding
- GO:0043560 insulin receptor substrate binding
- GO:0005143 interleukin-12 receptor binding
- GO:0046872 metal ion binding
- GO:0004715 non-membrane spanning protein tyrosine kinase activity
- GO:0051428 peptide hormone receptor binding
- GO:0043548 phosphatidylinositol 3-kinase binding
- GO:0004672 protein kinase activity
- GO:0019901 protein kinase binding
- GO:0004713 protein tyrosine kinase activity
- GO:0042169 SH2 domain binding
- GO:0030546 signaling receptor activator activity
- GO:0005102 signaling receptor binding
- GO:0031702 type 1 angiotensin receptor binding
- GO:0030041 actin filament polymerization
- GO:0042976 activation of Janus kinase activity
- GO:0002250 adaptive immune response
- GO:0006915 apoptotic process
- GO:0031103 axon regeneration
- GO:0007155 cell adhesion
- GO:0030154 cell differentiation
- GO:0007259 cell surface receptor signaling pathway via JAK-STAT
- GO:0038065 collagen-activated signaling pathway
- GO:0019221 cytokine-mediated signaling pathway
- GO:0007167 enzyme-linked receptor protein signaling pathway
- GO:0030218 erythrocyte differentiation
- GO:0038162 erythropoietin-mediated signaling pathway
- GO:0097191 extrinsic apoptotic signaling pathway
- GO:0038157 granulocyte-macrophage colony-stimulating factor signaling pathway
- GO:0060396 growth hormone receptor signaling pathway
- GO:0060397 growth hormone receptor signaling pathway via JAK-STAT
- GO:0035722 interleukin-12-mediated signaling pathway
- GO:0038155 interleukin-23-mediated signaling pathway
- GO:0038156 interleukin-3-mediated signaling pathway
- GO:0070757 interleukin-35-mediated signaling pathway
- GO:0038043 interleukin-5-mediated signaling pathway
- GO:0070102 interleukin-6-mediated signaling pathway
- GO:0035556 intracellular signal transduction
- GO:0008631 intrinsic apoptotic signaling pathway in response to oxidative stress
- GO:0031663 lipopolysaccharide-mediated signaling pathway
- GO:0061180 mammary gland epithelium development
- GO:0007498 mesoderm development
- GO:0001774 microglial cell activation
- GO:0050804 modulation of chemical synaptic transmission
- GO:0010667 negative regulation of cardiac muscle cell apoptotic process
- GO:0008285 negative regulation of cell population proliferation
- GO:0022408 negative regulation of cell-cell adhesion
- GO:1900016 negative regulation of cytokine production involved in inflammatory response
- GO:0043524 negative regulation of neuron apoptotic process
- GO:0120186 negative regulation of protein localization to chromatin
- GO:0031959 nuclear receptor-mediated mineralocorticoid signaling pathway
- GO:0048008 platelet-derived growth factor receptor signaling pathway
- GO:0045597 positive regulation of cell differentiation
- GO:0030335 positive regulation of cell migration
- GO:0010811 positive regulation of cell-substrate adhesion
- GO:0120162 positive regulation of cold-induced thermogenesis
- GO:0007204 positive regulation of cytosolic calcium ion concentration
- GO:1904037 positive regulation of epithelial cell apoptotic process
- GO:1902728 positive regulation of growth factor dependent skeletal muscle satellite cell proliferation
- GO:0060399 positive regulation of growth hormone receptor signaling pathway
- GO:0032024 positive regulation of insulin secretion
- GO:0032731 positive regulation of interleukin-1 beta production
- GO:0070665 positive regulation of leukocyte proliferation
- GO:0043410 positive regulation of MAPK cascade
- GO:0045348 positive regulation of MHC class II biosynthetic process
- GO:0045429 positive regulation of nitric oxide biosynthetic process
- GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- GO:0010572 positive regulation of platelet activation
- GO:1901731 positive regulation of platelet aggregation
- GO:0042307 positive regulation of protein import into nucleus
- GO:0060391 positive regulation of SMAD protein signal transduction
- GO:0042102 positive regulation of T cell proliferation
- GO:0045944 positive regulation of transcription by RNA polymerase II
- GO:0032760 positive regulation of tumor necrosis factor production
- GO:0042531 positive regulation of tyrosine phosphorylation of STAT protein
- GO:1904707 positive regulation of vascular associated smooth muscle cell proliferation
- GO:0035166 post-embryonic hemopoiesis
- GO:0043687 post-translational protein modification
- GO:0046777 protein autophosphorylation
- GO:0046634 regulation of alpha-beta T cell activation
- GO:0042981 regulation of apoptotic process
- GO:0050727 regulation of inflammatory response
- GO:0045428 regulation of nitric oxide biosynthetic process
- GO:1905539 regulation of postsynapse to nucleus signaling pathway
- GO:0046425 regulation of receptor signaling pathway via JAK-STAT
- GO:0046677 response to antibiotic
- GO:0033194 response to hydroperoxide
- GO:0070671 response to interleukin-12
- GO:0034612 response to tumor necrosis factor
- GO:0007165 signal transduction
- GO:0038163 thrombopoietin-mediated signaling pathway
- GO:0033209 tumor necrosis factor-mediated signaling pathway
- GO:0060333 type II interferon-mediated signaling pathway
Disease associations
- primary myelofibrosis MONDO:0009692
- acquired polycythemia vera MONDO:0009891
- Budd-Chiari syndrome MONDO:0010947
- acute myeloid leukemia MONDO:0018874
- thrombocythemia 3 MONDO:0013794
Drugs targeting this protein · 29
- MOMELOTINIB inhibitor
- AZD-1480 inhibitor
- FEDRATINIB inhibitor
- RUXOLITINIB PHOSPHATE inhibitor
- ZOTIRACICLIB inhibitor
- CT-1578 inhibitor
- PACRITINIB inhibitor
- TOFACITINIB CITRATE inhibitor
- BARICITINIB inhibitor
- GANDOTINIB inhibitor
- PEFICITINIB inhibitor
- FILGOTINIB inhibitor
- BMS-911543 inhibitor
- AC-430 inhibitor
- XL-019 inhibitor
- FEDRATINIB HYDROCHLORIDE inhibitor
- DELGOCITINIB inhibitor
- FILGOTINIB MALEATE inhibitor
- NS-018 inhibitor
- GUSACITINIB inhibitor
- DEURUXOLITINIB PHOSPHATE inhibitor
- IZENCITINIB inhibitor
- NEZULCITINIB inhibitor
- AT-9283 inhibitor
- LS-104 inhibitor
- PACRITINIB CITRATE inhibitor
- UPADACITINIB HEMIHYDRATE inhibitor
- LESTAURTINIB inhibitor
- MOMELOTINIB DIHYDROCHLORIDE MONOHYDRATE inhibitor
Related proteins · sequence + function similarity
- Tyrosine-protein kinase JAK2 1.00
- Tyrosine-protein kinase JAK2 1.00
- Tyrosine-protein kinase JAK2 0.99
- Tyrosine-protein kinase JAK2 0.99
- Tyrosine-protein kinase JAK2 0.98
- Tyrosine-protein kinase JAK1 0.93
- Tyrosine-protein kinase JAK1 0.93
- Tyrosine-protein kinase JAK1 0.92
- Tyrosine-protein kinase JAK1 0.90
- Tyrosine-protein kinase hopscotch 0.83
- Dual specificity protein kinase shkC 0.79
- Tyrosine-protein kinase SPK-1 0.76
Co-cited proteins · studied together in the literature
- Pericentriolar material 1 protein 5 shared papers
- Tyrosine-protein kinase JAK3 2 shared papers
- Interferon gamma receptor 2 2 shared papers
- Potassium voltage-gated channel subfamily A member 3 1 shared papers
- Interferon gamma receptor 1 2 shared papers
- Regulator of hemoglobinization and erythroid cell expansion protein 1 shared papers
- Tyrosine-protein kinase JAK2 3 shared papers
- Transcription factor ETV6 1 shared papers
- Suppressor of cytokine signaling 2 1 shared papers
- Rho guanine nucleotide exchange factor 1 1 shared papers
- Thrombopoietin receptor 1 shared papers
- Signal transducing adapter molecule 2 1 shared papers
Literature · 42 cited papers
- Up-regulation of Kv1.3 channels by janus kinase 2. J. Membr. Biol. · 2015
- RHEX, a novel regulator of human erythroid progenitor cell expansion and erythroblast development. J. Exp. Med. · 2014
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- Germline JAK2 mutation in a family with hereditary thrombocytosis. N. Engl. J. Med. · 2012
- Phosphorylation of p27Kip1 by JAK2 directly links cytokine receptor signaling to cell cycle control. Oncogene · 2011
- Signaling by vitamin A and retinol-binding protein regulates gene expression to inhibit insulin responses. Proc. Natl. Acad. Sci. U.S.A. · 2011
- Notch-induced Asb2 expression promotes protein ubiquitination by forming non-canonical E3 ligase complexes. Cell Res. · 2011
- Heme controls the regulation of protein tyrosine kinases Jak2 and Src. Biochem. Biophys. Res. Commun. · 2010
- Stat1 mediates an auto-regulation of hsp90beta gene in heat shock response. Cell. Signal. · 2010
- The Rho exchange factor Arhgef1 mediates the effects of angiotensin II on vascular tone and blood pressure. Nat. Med. · 2010
- JAK2 phosphorylates histone H3Y41 and excludes HP1alpha from chromatin. Nature · 2009
- Janus kinases in immune cell signaling. Immunol. Rev. · 2009
- … and 30 more in the literature graph