Entry Database : PDB / ID : 5tx5 Structure visualization Downloads & linksTitle Rip1 Kinase ( flag 1-294, C34A, C127A, C233A, C240A) with GSK772 ComponentsReceptor-interacting serine/threonine-protein kinase 1 Details Keywords transferase/transferase inhibitor / kinase domain Inhibitor necrosis / transferase-transferase inhibitor complexFunction / homology Function and homology informationFunction Domain/homology Component
regulation of ATP:ADP antiporter activity / ripoptosome assembly / positive regulation of interleukin-6-mediated signaling pathway / positive regulation of miRNA processing / ripoptosome assembly involved in necroptotic process / death domain binding / ripoptosome / Defective RIPK1-mediated regulated necrosis / TRIF-mediated programmed cell death / TLR3-mediated TICAM1-dependent programmed cell death ... regulation of ATP:ADP antiporter activity / ripoptosome assembly / positive regulation of interleukin-6-mediated signaling pathway / positive regulation of miRNA processing / ripoptosome assembly involved in necroptotic process / death domain binding / ripoptosome / Defective RIPK1-mediated regulated necrosis / TRIF-mediated programmed cell death / TLR3-mediated TICAM1-dependent programmed cell death / Microbial modulation of RIPK1-mediated regulated necrosis / Regulation by c-FLIP / CASP8 activity is inhibited / Dimerization of procaspase-8 / programmed necrotic cell death / TNF signaling / Caspase activation via Death Receptors in the presence of ligand / T cell apoptotic process / SARS-CoV-1-mediated effects on programmed cell death / positive regulation of macrophage differentiation / necroptotic signaling pathway / JUN kinase kinase kinase activity / peptidyl-serine autophosphorylation / NF-kB activation through FADD/RIP-1 pathway mediated by caspase-8 and -10 / positive regulation of necroptotic process / RIP-mediated NFkB activation via ZBP1 / death-inducing signaling complex / negative regulation of necroptotic process / positive regulation of tumor necrosis factor-mediated signaling pathway / death receptor binding / positive regulation of extrinsic apoptotic signaling pathway / positive regulation of programmed cell death / TRP channels / positive regulation of programmed necrotic cell death / TNFR1-induced proapoptotic signaling / RIPK1-mediated regulated necrosis / positive regulation of execution phase of apoptosis / necroptotic process / negative regulation of extrinsic apoptotic signaling pathway in absence of ligand / response to tumor necrosis factor / signaling adaptor activity / extrinsic apoptotic signaling pathway / negative regulation of canonical NF-kappaB signal transduction / tumor necrosis factor-mediated signaling pathway / TICAM1, RIP1-mediated IKK complex recruitment / IKK complex recruitment mediated by RIP1 / TNFR1-induced NF-kappa-B signaling pathway / positive regulation of interleukin-8 production / negative regulation of extrinsic apoptotic signaling pathway / Regulation of TNFR1 signaling / positive regulation of JNK cascade / protein catabolic process / Regulation of necroptotic cell death / cellular response to growth factor stimulus / cellular response to hydrogen peroxide / positive regulation of inflammatory response / positive regulation of non-canonical NF-kappaB signal transduction / positive regulation of tumor necrosis factor production / positive regulation of reactive oxygen species metabolic process / positive regulation of neuron apoptotic process / Ovarian tumor domain proteases / cellular response to tumor necrosis factor / positive regulation of NF-kappaB transcription factor activity / positive regulation of canonical NF-kappaB signal transduction / response to oxidative stress / amyloid fibril formation / Potential therapeutics for SARS / protein autophosphorylation / receptor complex / non-specific serine/threonine protein kinase / endosome membrane / Ub-specific processing proteases / protein kinase activity / intracellular signal transduction / inflammatory response / positive regulation of protein phosphorylation / positive regulation of apoptotic process / protein serine kinase activity / protein serine/threonine kinase activity / apoptotic process / ubiquitin protein ligase binding / protein-containing complex binding / positive regulation of gene expression / negative regulation of apoptotic process / protein homodimerization activity / positive regulation of transcription by RNA polymerase II / protein-containing complex / mitochondrion / ATP binding / identical protein binding / plasma membrane / cytosol Similarity search - Function RIP1, Death domain / Death domain profile. / DEATH domain, found in proteins involved in cell death (apoptosis). / Death domain / Death domain / Death-like domain superfamily / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 ... RIP1, Death domain / Death domain profile. / DEATH domain, found in proteins involved in cell death (apoptosis). / Death domain / Death domain / Death-like domain superfamily / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / 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. / Serine/Threonine protein kinases, catalytic domain / 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 : 2.56 Å DetailsAuthors Campobasso, N. / Ward, P. / Thrope, J. CitationJournal : J. Med. Chem. / Year : 2017Title : Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.Authors: Harris, P.A. / Berger, S.B. / Jeong, J.U. / Nagilla, R. / Bandyopadhyay, D. / Campobasso, N. / Capriotti, C.A. / Cox, J.A. / Dare, L. / Dong, X. / Eidam, P.M. / Finger, J.N. / Hoffman, S.J. ... Authors : Harris, P.A. / Berger, S.B. / Jeong, J.U. / Nagilla, R. / Bandyopadhyay, D. / Campobasso, N. / Capriotti, C.A. / Cox, J.A. / Dare, L. / Dong, X. / Eidam, P.M. / Finger, J.N. / Hoffman, S.J. / Kang, J. / Kasparcova, V. / King, B.W. / Lehr, R. / Lan, Y. / Leister, L.K. / Lich, J.D. / MacDonald, T.T. / Miller, N.A. / Ouellette, M.T. / Pao, C.S. / Rahman, A. / Reilly, M.A. / Rendina, A.R. / Rivera, E.J. / Schaeffer, M.C. / Sehon, C.A. / Singhaus, R.R. / Sun, H.H. / Swift, B.A. / Totoritis, R.D. / Vossenkamper, A. / Ward, P. / Wisnoski, D.D. / Zhang, D. / Marquis, R.W. / Gough, P.J. / Bertin, J. History Deposition Nov 15, 2016 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Jul 5, 2017 Provider : repository / Type : Initial releaseRevision 1.1 Mar 6, 2024 Group : Advisory / Data collection / Database referencesCategory : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_unobs_or_zero_occ_atoms Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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