Entry | Database: PDB / ID: 5kzi |
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Title | Crystal structure of human Pim-1 kinase in complex with an imidazopyridazine inhibitor. |
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Components | Serine/threonine-protein kinase pim-1 |
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Keywords | transferase/transferase inhibitor / TRANSFERASE / serine/threonine protein kinase / transferase-transferase inhibitor complex |
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Function / homology | Function and homology information
positive regulation of cardioblast proliferation / regulation of hematopoietic stem cell proliferation / cellular detoxification / vitamin D receptor signaling pathway / STAT5 activation downstream of FLT3 ITD mutants / transcription factor binding / positive regulation of cyclin-dependent protein serine/threonine kinase activity / ribosomal small subunit binding / positive regulation of cardiac muscle cell proliferation / positive regulation of TORC1 signaling ...positive regulation of cardioblast proliferation / regulation of hematopoietic stem cell proliferation / cellular detoxification / vitamin D receptor signaling pathway / STAT5 activation downstream of FLT3 ITD mutants / transcription factor binding / positive regulation of cyclin-dependent protein serine/threonine kinase activity / ribosomal small subunit binding / positive regulation of cardiac muscle cell proliferation / positive regulation of TORC1 signaling / Signaling by FLT3 fusion proteins / negative regulation of innate immune response / positive regulation of brown fat cell differentiation / protein serine/threonine kinase activator activity / regulation of transmembrane transporter activity / positive regulation of protein serine/threonine kinase activity / negative regulation of DNA-binding transcription factor activity / cellular response to type II interferon / manganese ion binding / Interleukin-4 and Interleukin-13 signaling / protein autophosphorylation / protein stabilization / non-specific serine/threonine protein kinase / cell cycle / protein phosphorylation / protein serine kinase activity / protein serine/threonine kinase activity / apoptotic process / nucleolus / negative regulation of apoptotic process / positive regulation of DNA-templated transcription / nucleoplasm / ATP binding / nucleus / plasma membrane / cytoplasm / cytosolSimilarity search - Function Serine/threonine-protein kinase pim-1/2/3 / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Serine/threonine-protein kinase, active site / Serine/Threonine protein kinases active-site signature. / Protein kinase domain / Serine/Threonine protein kinases, catalytic domain / Protein kinase, ATP binding site ...Serine/threonine-protein kinase pim-1/2/3 / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Serine/threonine-protein kinase, active site / Serine/Threonine protein kinases active-site signature. / Protein kinase domain / Serine/Threonine protein kinases, catalytic domain / 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: 2.1 Å |
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Authors | Mohr, C. |
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Citation | Journal: Bioorg. Med. Chem. Lett. / Year: 2016 Title: Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors. Authors: Wurz, R.P. / Sastri, C. / D'Amico, D.C. / Herberich, B. / Jackson, C.L. / Pettus, L.H. / Tasker, A.S. / Wu, B. / Guerrero, N. / Lipford, J.R. / Winston, J.T. / Yang, Y. / Wang, P. / Nguyen, ...Authors: Wurz, R.P. / Sastri, C. / D'Amico, D.C. / Herberich, B. / Jackson, C.L. / Pettus, L.H. / Tasker, A.S. / Wu, B. / Guerrero, N. / Lipford, J.R. / Winston, J.T. / Yang, Y. / Wang, P. / Nguyen, Y. / Andrews, K.L. / Huang, X. / Lee, M.R. / Mohr, C. / Zhang, J.D. / Reid, D.L. / Xu, Y. / Zhou, Y. / Wang, H.L. |
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History | Deposition | Jul 25, 2016 | Deposition site: RCSB / Processing site: RCSB |
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Revision 1.0 | Nov 9, 2016 | Provider: repository / Type: Initial release |
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Revision 1.1 | Dec 28, 2016 | Group: Database references |
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Revision 1.2 | Mar 6, 2024 | Group: Data collection / Database references / Category: chem_comp_atom / chem_comp_bond / database_2 Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession |
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