20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue ChemMedChem Année : 2010

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

Résumé

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.

Domaines

Chimie organique

Dates et versions

hal-00842680 , version 1 (09-07-2013)

Identifiants

Citer

Michael Groll, Nerea Gallastegui, Xavier Maréchal, Virginie Le Ravalec, Nicolas Basse, et al.. 20S proteasome inhibition: designing noncovalent linear peptide mimics of the natural product TMC-95A.. ChemMedChem, 2010, 5 (10), pp.1701-5. ⟨10.1002/cmdc.201000293⟩. ⟨hal-00842680⟩
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