Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11

Jing Li, Tanya Yakushi,Francesco Parlati,Andrew L Mackinnon,Christian Perez,Yuyong Ma,Kyle P Carter,Sharon Colayco, Gavin Magnuson, Brock Brown,Kevin Nguyen,Stefan Vasile,Eigo Suyama,Layton H Smith,Eduard Sergienko,Anthony B Pinkerton,Thomas D Y Chung,Amy E Palmer,Ian Pass,Sonja Hess,Seth M Cohen,Raymond J Deshaies

NATURE CHEMICAL BIOLOGY（2017）

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摘要

Two screening approaches converge on capzimin, a first-in-class inhibitor of the Rpn11 protease component of the 19S proteasome. Capzimin stabilizes polyubiquitinated substrates, induces the unfolded protein response, and blocks proliferation of cancer cells.

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关键词

Target identification,Screening,Small molecules,Metalloproteins,Post-translational modifications

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