Crystal structure of a covalently linked Aurora-A-MYCN complex

Diebold Mathias; Schoenemann Lars; Eilers MartinSotriffer ChristophSchindelin Hermann

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Crystal structure of a covalently linked Aurora-A-MYCN complex

机译：共价连接的Aurora-A-MYCN复合物的晶体结构

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Formation of the Aurora-A-MYCN complex increases levels of the oncogenic transcription factor MYCN in neuroblastoma cells by abrogating its degradation through the ubiquitin proteasome system. While some small-molecule inhibitors of Aurora-A were shown to destabilize MYCN, clinical trials have not been satisfactory to date. MYCN itself is considered to be `undruggable' due to its large intrinsically disordered regions. Targeting the Aurora-A-MYCN complex rather than Aurora-A or MYCN alone will open new possibilities for drug development and screening campaigns. To overcome the challenges that a ternary system composed of Aurora-A, MYCN and a small molecule entails, a covalently cross-linked construct of the Aurora-A-MYCN complex was designed, expressed and characterized, thus enabling screening and design campaigns to identify selective binders.

机译：形成Aurora-A-MYCN复杂的增加MYCN转录水平的致癌因素在神经母细胞瘤细胞通过废除它通过泛素蛋白酶体降解系统。Aurora-A被证明破坏MYCN,临床试验还没有令人满意的。本身被认为是无药可治”的原因其庞大的内在无序区域。而不是针对Aurora-A-MYCN复杂Aurora-A或独自MYCN将打开新的药物开发和筛选的可能性运动。组成的三元体系Aurora-A MYCN和小分子需要,一个共价交联Aurora-A-MYCN复杂的构造设计,表达和特征,从而使筛选和设计活动确定选择绑定。

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来源
《Acta crystallographica. Section D, Structural biology》 |2023年第1期|1-9|共9页
作者
Diebold Mathias; Schoenemann Lars; Eilers MartinSotriffer ChristophSchindelin Hermann;
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作者单位

University of Wurzburg,Univ Wurzburg;

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正文语种英语
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关键词
Aurora-A; MYCN; cross-linking; neuroblastoma cells; oncogenic transcription factors; cancer targets; N-MYC; HYDROLYSIS; INHIBITOR;

机译：极光-A;MYCN;交联;神经母细胞瘤细胞;致癌转录因子;癌症靶点;N-MYC;水解;抑制剂;

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Crystal structure of a covalently linked Aurora-A-MYCN complex

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