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:	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:	https://orca.cardiff.ac.uk/id/eprint/32208

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