登録情報 データベース : PDB / ID : 4zth 構造の表示 ダウンロードとリンクタイトル Structure of human p38aMAPK-arylpyridazinylpyridine fragment complex used in inhibitor discovery 要素Mitogen-activated protein kinase 14 詳細 キーワード TRANSFERASE機能・相同性 機能・相同性情報分子機能 ドメイン・相同性 構成要素
positive regulation of cyclase activity / stress-activated protein kinase signaling cascade / Activation of PPARGC1A (PGC-1alpha) by phosphorylation / CD163 mediating an anti-inflammatory response / regulation of synaptic membrane adhesion / stress-induced premature senescence / cell surface receptor protein serine/threonine kinase signaling pathway / 3'-UTR-mediated mRNA stabilization / KSRP (KHSRP) binds and destabilizes mRNA / cartilage condensation ... positive regulation of cyclase activity / stress-activated protein kinase signaling cascade / Activation of PPARGC1A (PGC-1alpha) by phosphorylation / CD163 mediating an anti-inflammatory response / regulation of synaptic membrane adhesion / stress-induced premature senescence / cell surface receptor protein serine/threonine kinase signaling pathway / 3'-UTR-mediated mRNA stabilization / KSRP (KHSRP) binds and destabilizes mRNA / cartilage condensation / positive regulation of myoblast fusion / cellular response to UV-B / Platelet sensitization by LDL / mitogen-activated protein kinase p38 binding / positive regulation of muscle cell differentiation / positive regulation of myotube differentiation / NFAT protein binding / Myogenesis / glucose import / Activation of the AP-1 family of transcription factors / negative regulation of hippo signaling / regulation of cytokine production involved in inflammatory response / ERK/MAPK targets / p38MAPK cascade / fatty acid oxidation / cellular response to lipoteichoic acid / MAP kinase kinase activity / response to dietary excess / response to muramyl dipeptide / RHO GTPases Activate NADPH Oxidases / MAP kinase activity / regulation of ossification / cellular response to vascular endothelial growth factor stimulus / mitogen-activated protein kinase / signal transduction in response to DNA damage / positive regulation of myoblast differentiation / chondrocyte differentiation / vascular endothelial growth factor receptor signaling pathway / stress-activated MAPK cascade / skeletal muscle tissue development / positive regulation of cardiac muscle cell proliferation / lipopolysaccharide-mediated signaling pathway / negative regulation of inflammatory response to antigenic stimulus / p38MAPK events / striated muscle cell differentiation / response to muscle stretch / positive regulation of interleukin-12 production / positive regulation of brown fat cell differentiation / osteoclast differentiation / positive regulation of erythrocyte differentiation / DNA damage checkpoint signaling / activated TAK1 mediates p38 MAPK activation / cellular response to ionizing radiation / positive regulation of glucose import / stem cell differentiation / NOD1/2 Signaling Pathway / response to insulin / bone development / negative regulation of canonical Wnt signaling pathway / placenta development / cell morphogenesis / platelet activation / cellular response to virus / VEGFA-VEGFR2 Pathway / spindle pole / positive regulation of protein import into nucleus / osteoblast differentiation / ADP signalling through P2Y purinoceptor 1 / glucose metabolic process / chemotaxis / positive regulation of reactive oxygen species metabolic process / cellular senescence / cellular response to tumor necrosis factor / peptidyl-serine phosphorylation / cellular response to lipopolysaccharide / protein phosphatase binding / angiogenesis / secretory granule lumen / Oxidative Stress Induced Senescence / Regulation of TP53 Activity through Phosphorylation / ficolin-1-rich granule lumen / transcription by RNA polymerase II / cell surface receptor signaling pathway / intracellular signal transduction / nuclear speck / protein serine kinase activity / protein serine/threonine kinase activity / glutamatergic synapse / apoptotic process / Neutrophil degranulation / positive regulation of gene expression / regulation of transcription by RNA polymerase II / enzyme binding / signal transduction / positive regulation of transcription by RNA polymerase II / mitochondrion / extracellular region / nucleoplasm / ATP binding / nucleus 類似検索 - 分子機能 Mitogen-activated protein kinase 14 / Mitogen-activated protein (MAP) kinase p38-like / : / 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 / Protein kinase domain ... Mitogen-activated protein kinase 14 / Mitogen-activated protein (MAP) kinase p38-like / : / 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 / 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 類似検索 - ドメイン・相同性 BETA-MERCAPTOETHANOL / 4-[3-(4-FLUOROPHENYL)-1H-PYRAZOL-4-YL]PYRIDINE / 6-chloro-3-phenyl-4-(pyridin-4-yl)pyridazine / Mitogen-activated protein kinase 14 類似検索 - 構成要素生物種 Homo sapiens (ヒト)手法 X線回折 / シンクロトロン / 分子置換 / 解像度 : 2.15 Å 詳細データ登録者 Grum-Tokars, V.L. / Roy, S.M. / Watterson, D.M. 資金援助 米国, 4件 詳細 詳細を隠す組織 認可番号 国 National Institutes of Health/National Institute of Neurological Disorders and Stroke (NIH/NINDS) U01AG043415 米国 National Institutes of Health/National Institute of Neurological Disorders and Stroke (NIH/NINDS) R01NS056051 米国 National Institutes of Health/National Institute of Neurological Disorders and Stroke (NIH/NINDS) R01AG031311 米国 National Institutes of Health/National Institute of Neurological Disorders and Stroke (NIH/NINDS) R01NS093920 米国
引用ジャーナル : J.Med.Chem. / 年 : 2019タイトル : A Selective and Brain Penetrant p38 alpha MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.著者 : Roy, S.M. / Minasov, G. / Arancio, O. / Chico, L.W. / Van Eldik, L.J. / Anderson, W.F. / Pelletier, J.C. / Watterson, D.M. 履歴 登録 2015年5月14日 登録サイト : RCSB / 処理サイト : RCSB改定 1.0 2016年6月22日 Provider : repository / タイプ : Initial release改定 1.1 2017年9月20日 Group : Author supporting evidence / Derived calculations / カテゴリ : pdbx_audit_support / pdbx_struct_oper_listItem : _pdbx_audit_support.funding_organization / _pdbx_struct_oper_list.symmetry_operation改定 1.2 2020年1月1日 Group : Author supporting evidence / Database referencesカテゴリ : citation / citation_author / pdbx_audit_supportItem : _citation.country / _citation.journal_abbrev ... _citation.country / _citation.journal_abbrev / _citation.journal_id_ASTM / _citation.journal_id_CSD / _citation.journal_id_ISSN / _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_DOI / _citation.pdbx_database_id_PubMed / _citation.title / _citation.year 改定 1.3 2024年3月6日 Group : Data collection / Database references / カテゴリ : chem_comp_atom / chem_comp_bond / database_2Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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