登録情報 | データベース: PDB / ID: 8udu |
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タイトル | The X-RAY co-crystal structure of human FGFR3 and Compound 17 |
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要素 | Fibroblast growth factor receptor 3 |
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キーワード | TRANSFERASE/INHIBITOR / FGFR inhibitor / Covalent Drug / alteration / mutation / structure-based drug design / kinase inhibitor / signaling / proliferation / TRANSFERASE / TRANSFERASE-INHIBITOR complex |
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機能・相同性 | 機能・相同性情報
fibroblast growth factor receptor apoptotic signaling pathway / t(4;14) translocations of FGFR3 / negative regulation of developmental growth / Signaling by FGFR3 fusions in cancer / bone maturation / chondrocyte proliferation / endochondral bone growth / FGFR3b ligand binding and activation / Signaling by activated point mutants of FGFR3 / FGFR3c ligand binding and activation ...fibroblast growth factor receptor apoptotic signaling pathway / t(4;14) translocations of FGFR3 / negative regulation of developmental growth / Signaling by FGFR3 fusions in cancer / bone maturation / chondrocyte proliferation / endochondral bone growth / FGFR3b ligand binding and activation / Signaling by activated point mutants of FGFR3 / FGFR3c ligand binding and activation / Phospholipase C-mediated cascade; FGFR3 / fibroblast growth factor receptor activity / endochondral ossification / positive regulation of phospholipase activity / bone morphogenesis / PI-3K cascade:FGFR3 / fibroblast growth factor binding / bone mineralization / cell surface receptor signaling pathway via JAK-STAT / PI3K Cascade / fibroblast growth factor receptor signaling pathway / chondrocyte differentiation / SHC-mediated cascade:FGFR3 / FRS-mediated FGFR3 signaling / positive regulation of tyrosine phosphorylation of STAT protein / transport vesicle / Signaling by FGFR3 in disease / skeletal system development / Negative regulation of FGFR3 signaling / receptor protein-tyrosine kinase / Constitutive Signaling by Aberrant PI3K in Cancer / MAPK cascade / PIP3 activates AKT signaling / cell-cell signaling / PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling / RAF/MAP kinase cascade / protein tyrosine kinase activity / positive regulation of MAPK cascade / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / positive regulation of ERK1 and ERK2 cascade / receptor complex / phosphorylation / positive regulation of cell population proliferation / Golgi apparatus / cell surface / endoplasmic reticulum / extracellular region / ATP binding / identical protein binding / plasma membrane類似検索 - 分子機能 Fibroblast growth factor receptor 3 transmembrane domain / Fibroblast growth factor receptor family / Immunoglobulin domain / 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. ...Fibroblast growth factor receptor 3 transmembrane domain / Fibroblast growth factor receptor family / Immunoglobulin domain / 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 / Immunoglobulin / Tyrosine-protein kinase, active site / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / 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類似検索 - ドメイン・相同性 |
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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: 1.737 Å |
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データ登録者 | Tyhonas, J.S. / Arnold, L.D. / Cox, J. / Franovic, A. / Gardiner, E. / Grandinetti, K. / Kania, R. / Kanouni, T. / Lardy, M. / Li, C. ...Tyhonas, J.S. / Arnold, L.D. / Cox, J. / Franovic, A. / Gardiner, E. / Grandinetti, K. / Kania, R. / Kanouni, T. / Lardy, M. / Li, C. / Martin, E.S. / Miller, N. / Mohan, A. / Murphy, E.A. / Perez, M. / Soroceanu, L. / Timple, N. / Uryu, S. / Womble, S. / Kaldor, S.W. |
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資金援助 | 1件 |
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引用 | ジャーナル: J.Med.Chem. / 年: 2024 タイトル: Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations. 著者: Tyhonas, J.S. / Arnold, L.D. / Cox, J.M. / Franovic, A. / Gardiner, E. / Grandinetti, K. / Kania, R. / Kanouni, T. / Lardy, M. / Li, C. / Martin, E.S. / Miller, N. / Mohan, A. / Murphy, E.A. ...著者: Tyhonas, J.S. / Arnold, L.D. / Cox, J.M. / Franovic, A. / Gardiner, E. / Grandinetti, K. / Kania, R. / Kanouni, T. / Lardy, M. / Li, C. / Martin, E.S. / Miller, N. / Mohan, A. / Murphy, E.A. / Perez, M. / Soroceanu, L. / Timple, N. / Uryu, S. / Womble, S. / Kaldor, S.W. |
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履歴 | 登録 | 2023年9月29日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2024年2月7日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2024年2月21日 | Group: Database references / カテゴリ: citation / citation_author Item: _citation.journal_volume / _citation.page_first ..._citation.journal_volume / _citation.page_first / _citation.page_last / _citation_author.identifier_ORCID |
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