Entry Database : PDB / ID : 4ra4 Structure visualization Downloads & linksTitle Crystal Structure of Human Protein Kinase C Alpha in Complex with Compound 28 ((R)-6-((3S,4S)-1,3-Dimethyl-piperidin-4-yl)-7-(2-fluoro-phenyl)-4-methyl-2,10-dihydro-9-oxa-1,2,4a-triaza-phenanthren-3-one) ComponentsProtein kinase C Details Keywords Transferase/transferase inhibitor / Kinase domain / Transferase-transferase inhibitor complexFunction / homology Function and homology informationFunction Domain/homology Component
Disinhibition of SNARE formation / Response to elevated platelet cytosolic Ca2+ / positive regulation of angiotensin-activated signaling pathway / response to phorbol 13-acetate 12-myristate / positive regulation of dense core granule biogenesis / regulation of primary metabolic process / calcium,diacylglycerol-dependent serine/threonine kinase activity / protein kinase C signaling / central nervous system neuron axonogenesis / diacylglycerol-dependent, calcium-independent serine/threonine kinase activity ... Disinhibition of SNARE formation / Response to elevated platelet cytosolic Ca2+ / positive regulation of angiotensin-activated signaling pathway / response to phorbol 13-acetate 12-myristate / positive regulation of dense core granule biogenesis / regulation of primary metabolic process / calcium,diacylglycerol-dependent serine/threonine kinase activity / protein kinase C signaling / central nervous system neuron axonogenesis / diacylglycerol-dependent, calcium-independent serine/threonine kinase activity / desmosome assembly / diacylglycerol binding / HuR (ELAVL1) binds and stabilizes mRNA / Trafficking of GluR2-containing AMPA receptors / Depolymerization of the Nuclear Lamina / WNT5A-dependent internalization of FZD4 / ROBO receptors bind AKAP5 / protein kinase C / Acetylcholine regulates insulin secretion / diacylglycerol-dependent serine/threonine kinase activity / mitotic nuclear membrane disassembly / negative regulation of glial cell apoptotic process / regulation of platelet aggregation / positive regulation of macrophage differentiation / alphav-beta3 integrin-PKCalpha complex / positive regulation of lipopolysaccharide-mediated signaling pathway / positive regulation of synapse assembly / Calmodulin induced events / Regulation of KIT signaling / positive regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway / response to corticosterone / Syndecan interactions / positive regulation of cardiac muscle hypertrophy / positive regulation of exocytosis / positive regulation of bone resorption / RET signaling / RHO GTPases Activate NADPH Oxidases / peptidyl-threonine phosphorylation / positive regulation of blood vessel endothelial cell migration / response to mechanical stimulus / positive regulation of endothelial cell proliferation / regulation of mRNA stability / EGFR Transactivation by Gastrin / negative regulation of cytokine production involved in inflammatory response / positive regulation of endothelial cell migration / positive regulation of cell adhesion / response to interleukin-1 / positive regulation of mitotic cell cycle / SHC1 events in ERBB2 signaling / histone H3T6 kinase activity / VEGFR2 mediated cell proliferation / response to reactive oxygen species / positive regulation of smooth muscle cell proliferation / apoptotic signaling pathway / Signaling by SCF-KIT / mitochondrial membrane / positive regulation of insulin secretion / response to peptide hormone / response to toxic substance / positive regulation of angiogenesis / G alpha (z) signalling events / integrin binding / Inactivation, recovery and regulation of the phototransduction cascade / response to estradiol / Ca2+ pathway / angiogenesis / response to ethanol / learning or memory / positive regulation of ERK1 and ERK2 cascade / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / protein kinase activity / cell adhesion / negative regulation of translation / intracellular signal transduction / protein phosphorylation / ciliary basal body / positive regulation of cell migration / protein serine kinase activity / protein serine/threonine kinase activity / apoptotic process / perinuclear region of cytoplasm / enzyme binding / endoplasmic reticulum / mitochondrion / extracellular exosome / zinc ion binding / nucleoplasm / ATP binding / nucleus / plasma membrane / cytosol / cytoplasm Similarity search - Function Classical Protein Kinase C alpha, catalytic domain / Protein kinase C, alpha/beta/gamma types / Protein kinase, C-terminal / Protein kinase C terminal domain / Diacylglycerol/phorbol-ester binding / Phorbol esters/diacylglycerol binding domain (C1 domain) / Zinc finger phorbol-ester/DAG-type signature. / Protein kinase C conserved region 2 (CalB) / C2 domain / Zinc finger phorbol-ester/DAG-type profile. ... Classical Protein Kinase C alpha, catalytic domain / Protein kinase C, alpha/beta/gamma types / Protein kinase, C-terminal / Protein kinase C terminal domain / Diacylglycerol/phorbol-ester binding / Phorbol esters/diacylglycerol binding domain (C1 domain) / Zinc finger phorbol-ester/DAG-type signature. / Protein kinase C conserved region 2 (CalB) / C2 domain / Zinc finger phorbol-ester/DAG-type profile. / Protein kinase C conserved region 1 (C1) domains (Cysteine-rich domains) / Protein kinase C-like, phorbol ester/diacylglycerol-binding domain / C2 domain / C2 domain profile. / C1-like domain superfamily / Extension to Ser/Thr-type protein kinases / AGC-kinase, C-terminal / AGC-kinase C-terminal domain profile. / C2 domain superfamily / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); 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 / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.63 Å DetailsAuthors Argiriadi, M.A. / George, D.M. CitationJournal : J.Med.Chem. / Year : 2015Title : Optimized Protein Kinase C theta (PKC theta ) Inhibitors Reveal Only Modest Anti-inflammatory Efficacy in a Rodent Model of Arthritis.Authors : George, D.M. / Breinlinger, E.C. / Argiriadi, M.A. / Zhang, Y. / Wang, J. / Bansal-Pakala, P. / Duignan, D.B. / Honore, P. / Lang, Q. / Mittelstadt, S. / Rundell, L. / Schwartz, A. / Sun, J. / Edmunds, J.J. History Deposition Sep 9, 2014 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Oct 8, 2014 Provider : repository / Type : Initial releaseRevision 1.1 Feb 4, 2015 Group : Database referencesRevision 1.2 Nov 22, 2017 Group : Refinement description / Category : softwareRevision 1.3 Mar 6, 2024 Group : Data collection / Database references ... Data collection / Database references / Derived calculations / Refinement description Category : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / software / struct_conn / struct_ref_seq_dif / struct_site Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession ... _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _software.name / _struct_conn.pdbx_leaving_atom_flag / _struct_ref_seq_dif.details / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id Revision 1.4 Nov 20, 2024 Group : Structure summary / Category : pdbx_entry_details / pdbx_modification_feature / Item : _pdbx_entry_details.has_protein_modification
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