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• W4313448089 abstract "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." @default.
• W4313448089 created "2023-01-06" @default.
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• W4313448089 date "2023-01-01" @default.
• W4313448089 modified "2023-10-18" @default.
• W4313448089 title "Crystal structure of a covalently linked Aurora-A–MYCN complex" @default.
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• W4313448089 doi "https://doi.org/10.1107/s2059798322011433" @default.
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