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M. Chem. Nerea Gallastegui, M. Sc. Philipp Beck, M. Sc. Marcelino Arciniega, Prof. Dr. Robert Huber, Stefan Hillebrand and Prof. Dr. Michael Groll Hydroxyureas as Noncovalent Proteasome Inhibitors Angewandte Chemie International Edition 51

Version of Record online: 21 NOV 2011 | DOI: 10.1002/anie.201106010

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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.

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