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8T5M

SOS2 crystal structure with fragment bound (compound 14)

8T5M の概要
エントリーDOI10.2210/pdb8t5m/pdb
分子名称Son of sevenless homolog 2, 1,2-ETHANEDIOL, SULFATE ION, ... (5 entities in total)
機能のキーワードsignaling protein
由来する生物種Homo sapiens (human)
タンパク質・核酸の鎖数1
化学式量合計58166.42
構造登録者
Gunn, R.J.,Lawson, J.D.,Ivetac, A.,Ulaganathan, T.,Coulombe, R.,Fethiere, J. (登録日: 2023-06-14, 公開日: 2024-01-10, 最終更新日: 2024-01-24)
主引用文献Smith, C.R.,Chen, D.,Christensen, J.G.,Coulombe, R.,Fethiere, J.,Gunn, R.J.,Hollander, J.,Jones, B.,Ketcham, J.M.,Khare, S.,Kuehler, J.,Lawson, J.D.,Marx, M.A.,Olson, P.,Pearson, K.E.,Ren, C.,Tsagris, D.,Ulaganathan, T.,Van't Veer, I.,Wang, X.,Ivetac, A.
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
J.Med.Chem., 67:774-781, 2024
Cited by
PubMed Abstract: SOS1 and SOS2 are guanine nucleotide exchange factors that mediate RTK-stimulated RAS activation. Selective SOS1:KRAS PPI inhibitors are currently under clinical investigation, whereas there are no reports to date of SOS2:KRAS PPI inhibitors. SOS2 activity is implicated in MAPK rebound when divergent SOS1 mutant cell lines are treated with the SOS1 inhibitor BI-3406; therefore, SOS2:KRAS inhibitors are of therapeutic interest. In this report, we detail a fragment-based screening strategy to identify X-ray cocrystal structures of five diverse fragment hits bound to SOS2.
PubMed: 38156904
DOI: 10.1021/acs.jmedchem.3c02140
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (1.79 Å)
構造検証レポート
Validation report summary of 8t5m
検証レポート(詳細版)ダウンロードをダウンロード

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件を2024-11-06に公開中

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