8PQH

PDGFRA T674I mutant kinase domain in complex with avapritinib

8PQH の概要

• エントリーDOI: 10.2210/pdb8pqh/pdb
• 分子名称: Platelet-derived growth factor receptor alpha, (1~{S})-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine, DI(HYDROXYETHYL)ETHER, ... (4 entities in total)
• 機能のキーワード: pdgfra protein kinase, avapritinib, inhibitor, tyrosine kinase, transmembrane receptor, platelet-derived growth factor receptor alpha, pdgf, platelet-derived growth factor, gist, gastrointestinal stromal tumors, gatekeeper mutant, p16234, transferase
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 40831.05

構造登録者

Teuber, A.,Kleinboelting, S.,Mueller, M.P.,Rauh, D. (登録日: 2023-07-11, 公開日: 2023-12-27, 最終更新日: 2024-03-13)

• 主引用文献: Teuber, A.,Schulz, T.,Fletcher, B.S.,Gontla, R.,Muhlenberg, T.,Zischinsky, M.L.,Niggenaber, J.,Weisner, J.,Kleinbolting, S.B.,Lategahn, J.,Sievers, S.,Muller, M.P.,Bauer, S.,Rauh, D.; Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA.; Nat Commun, 15:63-63, 2024; PubMed: 38167404; DOI: 10.1038/s41467-023-44376-8

実験手法

X-RAY DIFFRACTION (2.5 Å)