Entry | Database: PDB / ID: 5lwn |
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Title | Crystal structure of JAK3 in complex with Compound 5 (FM409) |
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Components | Tyrosine-protein kinase JAK3 |
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Keywords | TRANSFERASE / JAK3 / covalent inhibitor / reversible covalent inhibitor / induced pocket / arginine pocket / Structural Genomics / Structural Genomics Consortium / SGC |
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Function / homology | Function and homology information
negative regulation of dendritic cell cytokine production / negative regulation of FasL production / response to interleukin-9 / response to interleukin-2 / response to interleukin-15 / response to interleukin-4 / negative regulation of T-helper 1 cell differentiation / Interleukin-9 signaling / Interleukin-21 signaling / interleukin-9-mediated signaling pathway ...negative regulation of dendritic cell cytokine production / negative regulation of FasL production / response to interleukin-9 / response to interleukin-2 / response to interleukin-15 / response to interleukin-4 / negative regulation of T-helper 1 cell differentiation / Interleukin-9 signaling / Interleukin-21 signaling / interleukin-9-mediated signaling pathway / interleukin-4-mediated signaling pathway / negative regulation of T cell activation / interleukin-2-mediated signaling pathway / regulation of T cell apoptotic process / negative regulation of interleukin-12 production / interleukin-15-mediated signaling pathway / tyrosine phosphorylation of STAT protein / negative regulation of thymocyte apoptotic process / Interleukin-15 signaling / Interleukin-2 signaling / regulation of receptor signaling pathway via JAK-STAT / growth hormone receptor binding / extrinsic component of plasma membrane / Signaling by ALK / Interleukin-20 family signaling / negative regulation of interleukin-10 production / enzyme-linked receptor protein signaling pathway / T cell homeostasis / extrinsic component of cytoplasmic side of plasma membrane / cell surface receptor signaling pathway via JAK-STAT / growth hormone receptor signaling pathway via JAK-STAT / Interleukin receptor SHC signaling / Interleukin-7 signaling / B cell differentiation / non-specific protein-tyrosine kinase / non-membrane spanning protein tyrosine kinase activity / peptidyl-tyrosine phosphorylation / cytokine-mediated signaling pathway / RAF/MAP kinase cascade / protein phosphatase binding / protein tyrosine kinase activity / Potential therapeutics for SARS / Interleukin-4 and Interleukin-13 signaling / regulation of apoptotic process / adaptive immune response / endosome / cell differentiation / cytoskeleton / intracellular signal transduction / protein phosphorylation / innate immune response / ATP binding / plasma membrane / cytosolSimilarity search - Function Tyrosine-protein kinase, non-receptor Jak3 / : / Tyrosine-protein kinase, non-receptor Jak/Tyk2 / JAK, FERM F2 lobe domain / FERM F1 lobe ubiquitin-like domain / JAK1-3/TYK2, pleckstrin homology-like domain / Jak1 pleckstrin homology-like domain / FERM F2 acyl-CoA binding protein-like domain / FERM F1 ubiquitin-like domain / FERM domain ...Tyrosine-protein kinase, non-receptor Jak3 / : / Tyrosine-protein kinase, non-receptor Jak/Tyk2 / JAK, FERM F2 lobe domain / FERM F1 lobe ubiquitin-like domain / JAK1-3/TYK2, pleckstrin homology-like domain / Jak1 pleckstrin homology-like domain / FERM F2 acyl-CoA binding protein-like domain / FERM F1 ubiquitin-like domain / FERM domain / FERM domain profile. / Band 4.1 domain / Band 4.1 homologues / Src homology 2 domains / SH2 domain / SH2 domain superfamily / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / Tyrosine-protein kinase, active site / PH-like domain superfamily / Serine-threonine/tyrosine-protein kinase, catalytic domain / Protein tyrosine and serine/threonine kinase / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Protein kinase, ATP binding site / Protein kinases ATP-binding region signature. / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha BetaSimilarity search - Domain/homology |
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Biological species | Homo sapiens (human) |
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Method | X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution: 1.6 Å |
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Authors | Chaikuad, A. / Forster, M. / Mukhopadhyay, S. / Kupinska, K. / Ellis, K. / Mahajan, P. / Burgess-Brown, N. / Edwards, A.M. / Arrowsmith, C.H. / Bountra, C. ...Chaikuad, A. / Forster, M. / Mukhopadhyay, S. / Kupinska, K. / Ellis, K. / Mahajan, P. / Burgess-Brown, N. / Edwards, A.M. / Arrowsmith, C.H. / Bountra, C. / Laufer, S.A. / Knapp, S. / Structural Genomics Consortium (SGC) |
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Citation | Journal: Cell Chem Biol / Year: 2016 Title: Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. Authors: Forster, M. / Chaikuad, A. / Bauer, S.M. / Holstein, J. / Robers, M.B. / Corona, C.R. / Gehringer, M. / Pfaffenrot, E. / Ghoreschi, K. / Knapp, S. / Laufer, S.A. |
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History | Deposition | Sep 18, 2016 | Deposition site: PDBE / Processing site: PDBE |
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Revision 1.0 | Oct 26, 2016 | Provider: repository / Type: Initial release |
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Revision 1.1 | Nov 30, 2016 | Group: Database references |
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