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5XLZ

The crystal structure of tubulin complexed with a benzylidene derivative of 9(10H)-anthracenone

5XLZ の概要
エントリーDOI10.2210/pdb5xlz/pdb
分子名称Tubulin alpha-1B chain, 10-[(4-methoxy-3-oxidanyl-phenyl)methylidene]anthracen-9-one, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ... (12 entities in total)
機能のキーワードinhibitor, tubulin, cell cycle
由来する生物種Rattus norvegicus (Rat)
詳細
細胞内の位置Cytoplasm, cytoskeleton: P81947 Q6B856
Golgi apparatus : P63043
タンパク質・核酸の鎖数6
化学式量合計265047.50
構造登録者
Yu, Y.,Chen, Q. (登録日: 2017-05-12, 公開日: 2017-11-22, 最終更新日: 2024-03-27)
主引用文献Cheng, J.,Wu, Y.,Wang, Y.,Wang, C.,Wang, Y.,Wu, C.,Zeng, S.,Yu, Y.,Chen, Q.
Structure of a benzylidene derivative of 9(10H)-anthracenone in complex with tubulin provides a rationale for drug design.
Biochem. Biophys. Res. Commun., 495:185-188, 2018
Cited by
PubMed Abstract: Microtubules are composed of αβ-tubulin heterodimers and have been treated as highly attractive targets for antitumor drugs. A broad range of agents bind to tubulin and interfere with microtubule assembly, including colchicine binding site inhibitors (CBSIs). Tubulin Polymerization Inhibitor I (TPI1), a benzylidene derivative of 9(10H)-anthracenone, is a CBSI that inhibits the assembly of microtubules. However, for a long time, the design and development of anthracenone family drugs have been hindered by the lack of structural information of the tubulin-agent complex. Here we report a 2.3 Å crystal structure of tubulin complexed with TPI1, the first structure of anthracenone family agents. This complex structure reveals the interactions between TPI1 and tubulin, and thus provides insights into the development of new anthracenone derivatives targeting the colchicine binding site.
PubMed: 29102632
DOI: 10.1016/j.bbrc.2017.10.104
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (2.298 Å)
構造検証レポート
Validation report summary of 5xlz
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2025-07-16に公開中

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