Entry Database : PDB / ID : 6dcg Structure visualization Downloads & linksTitle Discovery of MK-8353: An Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology ComponentsMitogen-activated protein kinase 1 Details Keywords TRANSFERASE/TRANSFERASE INHIBITOR / KINASE INHIBITOR / KINASE SELECTIVITY / TRANSFERASE / SERINE/ THREONINE-PROTEIN KINASE / MAP KINASE / TRANSFERASE-TRANSFERASE INHIBITOR COMPLEXFunction / homology Function and homology informationFunction Domain/homology Component
phospho-PLA2 pathway / RAF-independent MAPK1/3 activation / MAPK1 (ERK2) activation / Signaling by NODAL / Frs2-mediated activation / ERK/MAPK targets / ERKs are inactivated / Activation of the AP-1 family of transcription factors / RHO GTPases Activate WASPs and WAVEs / IFNG signaling activates MAPKs ... phospho-PLA2 pathway / RAF-independent MAPK1/3 activation / MAPK1 (ERK2) activation / Signaling by NODAL / Frs2-mediated activation / ERK/MAPK targets / ERKs are inactivated / Activation of the AP-1 family of transcription factors / RHO GTPases Activate WASPs and WAVEs / IFNG signaling activates MAPKs / Negative feedback regulation of MAPK pathway / Gastrin-CREB signalling pathway via PKC and MAPK / Estrogen-dependent nuclear events downstream of ESR-membrane signaling / Golgi Cisternae Pericentriolar Stack Reorganization / Regulation of actin dynamics for phagocytic cup formation / Estrogen-stimulated signaling through PRKCZ / Growth hormone receptor signaling / Spry regulation of FGF signaling / SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription / Oxidative Stress Induced Senescence / Senescence-Associated Secretory Phenotype (SASP) / Oncogene Induced Senescence / Signaling by Activin / Downregulation of SMAD2/3:SMAD4 transcriptional activity / Signal attenuation / NCAM signaling for neurite out-growth / Negative regulation of FGFR1 signaling / Negative regulation of FGFR3 signaling / Negative regulation of FGFR4 signaling / Regulation of the apoptosome activity / Signal transduction by L1 / Negative regulation of FGFR2 signaling / RHO GTPases Activate NADPH Oxidases / Negative regulation of MAPK pathway / PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling / Interferon gamma signaling / FCERI mediated MAPK activation / Regulation of HSF1-mediated heat shock response / MAP2K and MAPK activation / Recycling pathway of L1 / neural crest cell development / diadenosine tetraphosphate biosynthetic process / cardiac neural crest cell development involved in heart development / caveolin-mediated endocytosis / cytosine metabolic process / response to epidermal growth factor / mitogen-activated protein kinase kinase kinase binding / positive regulation of macrophage proliferation / outer ear morphogenesis / regulation of cellular pH / regulation of Golgi inheritance / Thrombin signalling through proteinase activated receptors (PARs) / RAF/MAP kinase cascade / ERBB signaling pathway / labyrinthine layer blood vessel development / mammary gland epithelial cell proliferation / trachea formation / Neutrophil degranulation / regulation of early endosome to late endosome transport / regulation of stress-activated MAPK cascade / : / positive regulation of macrophage chemotaxis / lung morphogenesis / ERBB2-ERBB3 signaling pathway / response to exogenous dsRNA / regulation of cytoskeleton organization / face development / progesterone receptor signaling pathway / androgen receptor signaling pathway / pseudopodium / negative regulation of cell differentiation / Bergmann glial cell differentiation / positive regulation of telomere capping / thyroid gland development / steroid hormone receptor signaling pathway / decidualization / MAP kinase activity / regulation of ossification / mitogen-activated protein kinase / phosphatase binding / Schwann cell development / stress-activated MAPK cascade / lipopolysaccharide-mediated signaling pathway / positive regulation of cardiac muscle cell proliferation / sensory perception of pain / positive regulation of telomere maintenance via telomerase / cellular response to cadmium ion / ERK1 and ERK2 cascade / cellular response to amino acid starvation / myelination / dendrite cytoplasm / phosphotyrosine residue binding / RNA polymerase II CTD heptapeptide repeat kinase activity / insulin-like growth factor receptor signaling pathway / thymus development / positive regulation of peptidyl-threonine phosphorylation / caveola / positive regulation of translation / long-term synaptic potentiation / animal organ morphogenesis Similarity search - Function Mitogen-activated protein (MAP) kinase, ERK1/2 / Mitogen-activated protein (MAP) kinase, conserved site / MAP kinase signature. / 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 ... Mitogen-activated protein (MAP) kinase, ERK1/2 / Mitogen-activated protein (MAP) kinase, conserved site / MAP kinase signature. / 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 Rattus norvegicus (Norway rat)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 1.45 Å DetailsAuthors Boga, S.B. / Deng, Y. / Zhu, L. / Nan, Y. / Cooper, A. / Shipps Jr., G.W. / Doll, R. / Shih, N. / Zhu, H. / Sun, R. ...Boga, S.B. / Deng, Y. / Zhu, L. / Nan, Y. / Cooper, A. / Shipps Jr., G.W. / Doll, R. / Shih, N. / Zhu, H. / Sun, R. / Wang, T. / Paliwal, S. / Tsui, H. / Gao, X. / Yao, X. / Desai, J. / Wang, J. / Alhassan, A.B. / Kelly, J. / Patel, M. / Muppalla, K. / Gudipati, S. / Zhang, L. / Buevich, A. / Hesk, D. / Carr, D. / Dayananth, P. / Mei, H. / Cox, K. / Sherborne, B. / Hruza, A.W. / Xiao, L. / Jin, W. / Long, B. / Liu, G. / Taylor, S.A. / Kirschmeier, P. / Windsor, W.T. / Bishop, R. / Samatar, A.A. CitationJournal : ACS Med Chem Lett / Year : 2018Title : MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.Authors: Boga, S.B. / Deng, Y. / Zhu, L. / Nan, Y. / Cooper, A.B. / Shipps Jr., G.W. / Doll, R. / Shih, N.Y. / Zhu, H. / Sun, R. / Wang, T. / Paliwal, S. / Tsui, H.C. / Gao, X. / Yao, X. / Desai, J. ... Authors : Boga, S.B. / Deng, Y. / Zhu, L. / Nan, Y. / Cooper, A.B. / Shipps Jr., G.W. / Doll, R. / Shih, N.Y. / Zhu, H. / Sun, R. / Wang, T. / Paliwal, S. / Tsui, H.C. / Gao, X. / Yao, X. / Desai, J. / Wang, J. / Alhassan, A.B. / Kelly, J. / Patel, M. / Muppalla, K. / Gudipati, S. / Zhang, L.K. / Buevich, A. / Hesk, D. / Carr, D. / Dayananth, P. / Black, S. / Mei, H. / Cox, K. / Sherborne, B. / Hruza, A.W. / Xiao, L. / Jin, W. / Long, B. / Liu, G. / Taylor, S.A. / Kirschmeier, P. / Windsor, W.T. / Bishop, R. / Samatar, A.A. History Deposition May 6, 2018 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Aug 8, 2018 Provider : repository / Type : Initial releaseRevision 1.1 Oct 11, 2023 Group : Data collection / Database references / Refinement descriptionCategory : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_initial_refinement_model Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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