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Hydroxyureas as Noncovalent Proteasome Inhibitors

Gallastegui, Nerea, Beck, Philipp, Arciniega, Marcelino, Huber, Robert, Hillebrand, Stefan and Groll, Michael 2012. Hydroxyureas as Noncovalent Proteasome Inhibitors. Angewandte Chemie - International Edition 51 (1) , pp. 247-249. 10.1002/anie.201106010

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Abstract

Inhibitors with a new mechanism of action are needed for 20S proteasome (CP) inhibition owing to the ineffectiveness of current market drugs against some types of solid tumors. A novel class of nonpeptidic CP inhibitors has been developed, which display reversible and noncovalent binding. The structure-based design of these highly active and site-specific inhibitors revealed unexplored binding subpockets.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Subjects: Q Science > Q Science (General)
Uncontrolled Keywords: hydroxyureas; inhibitors; lipoxygenases; proteasomes; protein crystallography
Publisher: Wiley-Blackwell
ISSN: 1433-7851
Last Modified: 24 Jun 2017 09:33
URI: http://orca-mwe.cf.ac.uk/id/eprint/32208

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