Discovery and characterization of highly potent and selective allosteric USP7 inhibitors

Gerald Gavory, Colin R O'Dowd,Matthew D Helm, Jakub Flasz, Elias Arkoudis,Anthony Dossang,Caroline Hughes, Eamon Cassidy,Keeva McClelland, Ewa Odrzywol,Natalie Page,Oliver Barker, Hugues Miel,Timothy Harrison

NATURE CHEMICAL BIOLOGY（2017）

引用 151|浏览7

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摘要

selective inhibitor of the deubiquitinase USP7 binds an allosteric site to inhibit its MDM2-stabilizing activity, resulting in stabilization of p53 and p21, which confers hypersensitivity to cancer cells for killing by the compound.

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关键词

Cancer,Chemical tools,Target validation,X-ray crystallography,Chemistry/Food Science,general,Biochemical Engineering,Biochemistry,Cell Biology,Bioorganic Chemistry

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