4RWK

Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M) in complex with N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE (AZD4547)

4RWK の概要

• エントリーDOI: 10.2210/pdb4rwk/pdb
• 関連するPDBエントリー: 4RWI 4RWJ 4RWL
• 分子名称: Fibroblast growth factor receptor 1, N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide, MAGNESIUM ION, ... (4 entities in total)
• 機能のキーワード: receptor tyrosine kinase, gatekeeper mutation, proto-oncogene, kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein: P11362
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 73468.78

構造登録者

Sohl, C.D.,Anderson, K.S. (登録日: 2014-12-04, 公開日: 2015-04-15, 最終更新日: 2023-09-20)

• 主引用文献: Sohl, C.D.,Ryan, M.R.,Luo, B.,Frey, K.M.,Anderson, K.S.; Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles' Heel of Targeted Therapy.; Acs Chem.Biol., 10:1319-1329, 2015; PubMed: 25686244; DOI: 10.1021/acschembio.5b00014

実験手法

X-RAY DIFFRACTION (2.982 Å)