Entry Database : PDB / ID : 6hx1 Structure visualization Downloads & linksTitle IRE1 ALPHA IN COMPLEX WITH imidazo[1,2-b]pyridazin-8-amine compound 2 ComponentsSerine/threonine-protein kinase/endoribonuclease IRE1 Details Keywords TRANSFERASE / IRE1 KINASE / PROTEROS BIOSTRUCTURES GMBHFunction / homology Function and homology informationFunction Domain/homology Component
peptidyl-serine trans-autophosphorylation / mRNA splicing, via endonucleolytic cleavage and ligation / AIP1-IRE1 complex / Ire1 complex / IRE1alpha activates chaperones / IRE1-TRAF2-ASK1 complex / insulin metabolic process / peptidyl-serine autophosphorylation / IRE1-RACK1-PP2A complex / platelet-derived growth factor receptor binding ... peptidyl-serine trans-autophosphorylation / mRNA splicing, via endonucleolytic cleavage and ligation / AIP1-IRE1 complex / Ire1 complex / IRE1alpha activates chaperones / IRE1-TRAF2-ASK1 complex / insulin metabolic process / peptidyl-serine autophosphorylation / IRE1-RACK1-PP2A complex / platelet-derived growth factor receptor binding / Hydrolases; Acting on ester bonds; Endoribonucleases producing 5'-phosphomonoesters / positive regulation of endoplasmic reticulum unfolded protein response / endothelial cell proliferation / nuclear inner membrane / IRE1-mediated unfolded protein response / mRNA catabolic process / intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress / cellular response to vascular endothelial growth factor stimulus / cellular response to unfolded protein / regulation of macroautophagy / positive regulation of JUN kinase activity / positive regulation of vascular associated smooth muscle cell proliferation / RNA endonuclease activity / Hsp70 protein binding / response to endoplasmic reticulum stress / positive regulation of RNA splicing / cellular response to glucose stimulus / Hsp90 protein binding / ADP binding / cellular response to hydrogen peroxide / unfolded protein binding / protein autophosphorylation / non-specific serine/threonine protein kinase / protein phosphorylation / protein serine kinase activity / protein serine/threonine kinase activity / endoplasmic reticulum membrane / enzyme binding / magnesium ion binding / endoplasmic reticulum / protein homodimerization activity / mitochondrion / ATP binding / identical protein binding / cytoplasm Similarity search - Function KEN domain / Serine/threonine-protein kinase/endoribonuclease IRE1/2-like / KEN domain / KEN domain superfamily / Ribonuclease 2-5A / KEN domain profile. / domain in protein kinases, N-glycanases and other nuclear proteins / de novo design (two linked rop proteins) / Pyrrolo-quinoline quinone beta-propeller repeat / beta-propeller repeat ... KEN domain / Serine/threonine-protein kinase/endoribonuclease IRE1/2-like / KEN domain / KEN domain superfamily / Ribonuclease 2-5A / KEN domain profile. / domain in protein kinases, N-glycanases and other nuclear proteins / de novo design (two linked rop proteins) / Pyrrolo-quinoline quinone beta-propeller repeat / beta-propeller repeat / Quinoprotein alcohol dehydrogenase-like superfamily / 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 / WD40/YVTN repeat-like-containing domain superfamily / Serine/Threonine protein kinases, catalytic domain / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily / Up-down Bundle / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha Beta Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.14 Å DetailsAuthors Augustin, M.A. / Krapp, S. / Bayliss, R. / Collins, I. Funding support United Kingdom, 1items Details Hide detailsOrganization Grant number Country Cancer Research UK C309/A11566 United Kingdom
CitationJournal : J.Med.Chem. / Year : 2019Title : Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1 alpha Kinase-Endoribonuclease.Authors: Colombano, G. / Caldwell, J.J. / Matthews, T.P. / Bhatia, C. / Joshi, A. / McHardy, T. / Mok, N.Y. / Newbatt, Y. / Pickard, L. / Strover, J. / Hedayat, S. / Walton, M.I. / Myers, S.M. / ... Authors : Colombano, G. / Caldwell, J.J. / Matthews, T.P. / Bhatia, C. / Joshi, A. / McHardy, T. / Mok, N.Y. / Newbatt, Y. / Pickard, L. / Strover, J. / Hedayat, S. / Walton, M.I. / Myers, S.M. / Jones, A.M. / Saville, H. / McAndrew, C. / Burke, R. / Eccles, S.A. / Davies, F.E. / Bayliss, R. / Collins, I. History Deposition Oct 15, 2018 Deposition site : PDBE / Processing site : PDBERevision 1.0 Feb 27, 2019 Provider : repository / Type : Initial releaseRevision 1.1 Mar 27, 2019 Group : Data collection / Database references / Category : citation / citation_author / pdbx_database_procItem : _citation.journal_abbrev / _citation.journal_id_ISSN ... _citation.journal_abbrev / _citation.journal_id_ISSN / _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.title / _citation_author.name Revision 1.2 Sep 25, 2019 Group : Data collection / Category : reflns / Item : _reflns.pdbx_Rmerge_I_obsRevision 1.3 Oct 30, 2019 Group : Data collection / Source and taxonomy / Structure summaryCategory : entity / entity_src_gen / pdbx_entity_src_syn / Item : _entity.src_methodRevision 1.4 Jan 24, 2024 Group : Advisory / Data collection ... Advisory / Data collection / Database references / Refinement description Category : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_initial_refinement_model / pdbx_unobs_or_zero_occ_atoms Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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