5XLZ
The crystal structure of tubulin complexed with a benzylidene derivative of 9(10H)-anthracenone
5XLZ の概要
エントリーDOI | 10.2210/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 | |
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: 29102632DOI: 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) |
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