Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53
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- 作者：Andreas C. Joerger1 ; andreas.joerger@gmx.de" class="auth_mail" title="E-mail the corresponding author ; Matthias R. Bauer1 ; Rainer Wilcken1 ; Matthias G.J. Baud1 ; Hannes Harbrecht1 ; Thomas E. Exner2 ; Frank M. Boeckler2 ; John Spencer3 ; Alan R. Fersht1
- 关键词：p53 ; mutant rescue ; drug design ; molecular chaperone ; transient protein states
- 刊名：Structure
- 出版年：2015
- 出版时间：1 December 2015
- 年：2015
- 卷：23
- 期：12
- 页码：2246-2255
- 全文大小：3274 K
文摘
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Surface crevice in the p53 cancer mutant Y220C targeted with small molecules
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Numerous high-resolution Y220C-ligand structures determined
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Transiently open hydrophobic subpocket identified
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Structures provide a framework for the design of potent binders for cancer therapy