Entry Database : PDB / ID : 5ipj Structure visualization Downloads & linksTitle Crystal structure of human Pim-1 kinase in complex with a quinazolinone-pyrrolopyrrolone inhibitor. ComponentsSerine/threonine-protein kinase pim-1 Details Keywords transferase/transferase inhibitor / TRANSFERASE / serine/threonine protein kinase / transferase-transferase inhibitor complexFunction / homology Function and homology informationFunction Domain/homology Component
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 / ribosomal small subunit binding / positive regulation of cyclin-dependent protein serine/threonine kinase activity / 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 / ribosomal small subunit binding / positive regulation of cyclin-dependent protein serine/threonine kinase activity / 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 / cytosol Similarity 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 Beta Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / MOLECULAR REPLACEMENT / Resolution : 2.1 Å DetailsAuthors Mohr, C. CitationJournal : J.Med.Chem. / Year : 2016Title : Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.Authors: Pettus, L.H. / Andrews, K.L. / Booker, S.K. / Chen, J. / Cee, V.J. / Chavez, F. / Chen, Y. / Eastwood, H. / Guerrero, N. / Herberich, B. / Hickman, D. / Lanman, B.A. / Laszlo, J. / Lee, M.R. ... Authors : Pettus, L.H. / Andrews, K.L. / Booker, S.K. / Chen, J. / Cee, V.J. / Chavez, F. / Chen, Y. / Eastwood, H. / Guerrero, N. / Herberich, B. / Hickman, D. / Lanman, B.A. / Laszlo, J. / Lee, M.R. / Lipford, J.R. / Mattson, B. / Mohr, C. / Nguyen, Y. / Norman, M.H. / Powers, D. / Reed, A.B. / Rex, K. / Sastri, C. / Tamayo, N. / Wang, P. / Winston, J.T. / Wu, B. / Wu, T. / Wurz, R.P. / Xu, Y. / Zhou, Y. / Tasker, A.S. / Wang, H.L. History Deposition Mar 9, 2016 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Jun 22, 2016 Provider : repository / Type : Initial releaseRevision 1.1 Jul 27, 2016 Group : Database referencesRevision 1.2 Mar 6, 2024 Group : Data collection / Database references / Derived calculationsCategory : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / citation / database_2 / pdbx_struct_oper_list Item : _citation.journal_id_CSD / _database_2.pdbx_DOI ... _citation.journal_id_CSD / _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_oper_list.symmetry_operation
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