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20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A

Groll, Michael, Gallastegui, Nerea, Maréchal, Xavier, Le Ravalec, Virginie, Basse, Nicolas, Richy, Nicolas, Genin, Emilie, Huber, Robert, Moroder, Luis, Vidal, Joëlle and Reboud-Ravaux, Michèle 2010. 20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A. ChemMedChem 5 (10) , pp. 1701-1705. 10.1002/cmdc.201000293

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Abstract

The 20S proteasome maintains homeostasis and regulates important intracellular processes by subjecting most intracellular proteins to endoproteolytic cleavage. This complex hydrolysis machinery has received considerable attention for the treatment of many diseases, including cancer. We report a new set of noncovalent peptide mimics based on TMC-95A and our rational approach to inhibitor optimization using both crystallographic and kinetic studies.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Subjects: Q Science > Q Science (General)
Publisher: John Wiley & Sons
ISSN: 1860-7179
Last Modified: 24 Jun 2017 08:42
URI: http://orca-mwe.cf.ac.uk/id/eprint/17747

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