登録情報 | データベース: PDB / ID: 3js2 |
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タイトル | Crystal structure of minimal kinase domain of fibroblast growth factor receptor 1 in complex with 5-(2-thienyl)nicotinic acid |
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要素 | Basic fibroblast growth factor receptor 1 |
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キーワード | TRANSFERASE (転移酵素) / fibroblast growth factor (線維芽細胞増殖因子) / receptor tyrosine kinase (受容体型チロシンキナーゼ) / inhibitor (酵素阻害剤) / thienyl nicotinic acid / Alternative splicing (選択的スプライシング) / ATP-binding / Chromosomal rearrangement / Craniosynostosis (頭蓋骨縫合早期癒合症) / Disease mutation / Disulfide bond (ジスルフィド) / Dwarfism (小人症) / Glycoprotein (糖タンパク質) / Heparin-binding / Hypogonadotropic hypogonadism / Immunoglobulin domain (免疫グロブリンフォールド) / Kallmann syndrome (カルマン症候群) / Kinase (キナーゼ) / Membrane (生体膜) / Nucleotide-binding / Phosphoprotein / Polymorphism / Receptor / Transmembrane (膜貫通型タンパク質) / Tyrosine-protein kinase |
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機能・相同性 | 機能・相同性情報
Signaling by FGFR1 amplification mutants / negative regulation of fibroblast growth factor production / positive regulation of mitotic cell cycle DNA replication / regulation of extrinsic apoptotic signaling pathway in absence of ligand / Signaling by plasma membrane FGFR1 fusions / diphosphate metabolic process / FGFR1c and Klotho ligand binding and activation / vitamin D3 metabolic process / regulation of phosphate transport / regulation of lateral mesodermal cell fate specification ...Signaling by FGFR1 amplification mutants / negative regulation of fibroblast growth factor production / positive regulation of mitotic cell cycle DNA replication / regulation of extrinsic apoptotic signaling pathway in absence of ligand / Signaling by plasma membrane FGFR1 fusions / diphosphate metabolic process / FGFR1c and Klotho ligand binding and activation / vitamin D3 metabolic process / regulation of phosphate transport / regulation of lateral mesodermal cell fate specification / positive regulation of MAPKKK cascade by fibroblast growth factor receptor signaling pathway / cementum mineralization / response to sodium phosphate / regulation of branching involved in salivary gland morphogenesis by mesenchymal-epithelial signaling / receptor-receptor interaction / fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex development / auditory receptor cell development / ventricular zone neuroblast division / Epithelial-Mesenchymal Transition (EMT) during gastrulation / positive regulation of parathyroid hormone secretion / chordate embryonic development / mesenchymal cell proliferation / paraxial mesoderm development / FGFR1b ligand binding and activation / fibroblast growth factor receptor activity / branching involved in salivary gland morphogenesis / Signaling by activated point mutants of FGFR1 / FGFR1c ligand binding and activation / organ induction / Downstream signaling of activated FGFR1 / Phospholipase C-mediated cascade: FGFR1 / positive regulation of phospholipase activity / lung-associated mesenchyme development / cell projection assembly / cellular response to fibroblast growth factor stimulus / outer ear morphogenesis / middle ear morphogenesis / embryonic limb morphogenesis / skeletal system morphogenesis / positive regulation of endothelial cell chemotaxis / positive regulation of mesenchymal cell proliferation / cardiac muscle cell proliferation / positive regulation of vascular endothelial cell proliferation / ureteric bud development / inner ear morphogenesis / midbrain development / fibroblast growth factor binding / positive regulation of stem cell proliferation / Formation of paraxial mesoderm / PI-3K cascade:FGFR1 / regulation of cell differentiation / phosphatidylinositol-mediated signaling / PI3K Cascade / 上皮間葉転換 / positive regulation of blood vessel endothelial cell migration / fibroblast growth factor receptor signaling pathway / calcium ion homeostasis / chondrocyte differentiation / : / SHC-mediated cascade:FGFR1 / cell maturation / positive regulation of cardiac muscle cell proliferation / FRS-mediated FGFR1 signaling / positive regulation of neuron differentiation / Signaling by FGFR1 in disease / NCAM signaling for neurite out-growth / SH2 domain binding / Signal transduction by L1 / skeletal system development / stem cell proliferation / 細胞分化 / positive regulation of cell differentiation / sensory perception of sound / Negative regulation of FGFR1 signaling / neuron migration / positive regulation of MAP kinase activity / 受容体型チロシンキナーゼ / positive regulation of neuron projection development / peptidyl-tyrosine phosphorylation / Constitutive Signaling by Aberrant PI3K in Cancer / neuron projection development / 分裂促進因子活性化タンパク質キナーゼ / 遊走 / PIP3 activates AKT signaling / heparin binding / 遺伝子発現 / PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling / cytoplasmic vesicle / RAF/MAP kinase cascade / protein tyrosine kinase activity / 血管新生 / in utero embryonic development / positive regulation of MAPK cascade / protein autophosphorylation / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / receptor complex / protein phosphorylation / positive regulation of cell population proliferation / negative regulation of transcription by RNA polymerase II / protein homodimerization activity類似検索 - 分子機能 Fibroblast growth factor receptor 1, catalytic domain / Fibroblast growth factor receptor family / 抗体 / 免疫グロブリンフォールド / Immunoglobulin I-set / Immunoglobulin I-set domain / Immunoglobulin subtype 2 / Immunoglobulin C-2 Type / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain ...Fibroblast growth factor receptor 1, catalytic domain / Fibroblast growth factor receptor family / 抗体 / 免疫グロブリンフォールド / Immunoglobulin I-set / Immunoglobulin I-set domain / Immunoglobulin subtype 2 / Immunoglobulin C-2 Type / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / Immunoglobulin subtype / 抗体 / Tyrosine-protein kinase, active site / 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 / Ig-like domain profile. / Immunoglobulin-like domain / Immunoglobulin-like domain superfamily / Protein kinase, ATP binding site / Protein kinases ATP-binding region signature. / Immunoglobulin-like fold / 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 リン酸塩 / 5-(2-thienyl)nicotinic acid / 線維芽細胞増殖因子受容体1類似検索 - 構成要素 |
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生物種 | Homo sapiens (ヒト) |
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手法 | X線回折 / シンクロトロン / 分子置換 / 解像度: 2.2 Å |
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データ登録者 | Bae, J.H. / Ravindranathan, K.P. / Mandiyan, V. / Ekkati, A.R. / Schlessinger, J. / Jorgensen, W.L. |
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引用 | ジャーナル: J.Med.Chem. / 年: 2010 タイトル: Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening 著者: Ravindranathan, K.P. / Mandiyan, V. / Ekkati, A.R. / Bae, J.H. / Schlessinger, J. / Jorgensen, W.L. |
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履歴 | 登録 | 2009年9月9日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2010年2月23日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2011年7月13日 | Group: Version format compliance |
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改定 1.2 | 2021年10月13日 | Group: Database references / Derived calculations / Structure summary カテゴリ: chem_comp / database_2 ...chem_comp / database_2 / struct_ref_seq_dif / struct_site Item: _chem_comp.pdbx_synonyms / _database_2.pdbx_DOI ..._chem_comp.pdbx_synonyms / _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _struct_ref_seq_dif.details / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id |
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改定 1.3 | 2023年2月1日 | Group: Database references / カテゴリ: struct_ref_seq_dif / Item: _struct_ref_seq_dif.details |
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改定 1.4 | 2023年9月20日 | Group: Data collection / Refinement description カテゴリ: chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model |
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