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Document type:
journal article 
Author(s):
Dubiella, Christian; Cui, Haissi; Gersch, Malte; Brouwer, Arwin J; Sieber, Stephan A; Krüger, Achim; Liskamp, Rob M J; Groll, Michael 
Title:
Selective inhibition of the immunoproteasome by ligand-induced crosslinking of the active site. 
Abstract:
The concept of proteasome inhibition ranks among the latest achievements in the treatment of blood cancer and represents a promising strategy for modulating autoimmune diseases. In this study, we describe peptidic sulfonyl fluoride inhibitors that selectively block the catalytic ?5 subunit of the immunoproteasome by inducing only marginal cytotoxic effects. Structural and mass spectrometric analyses revealed a novel reaction mechanism involving polarity inversion and irreversible crosslinking of...    »
 
Journal title abbreviation:
Angew Chem Int Ed Engl 
Year:
2014 
Journal volume:
53 
Journal issue:
44 
Pages contribution:
11969-73 
Language:
eng 
Print-ISSN:
0570-0833 
TUM Institution:
Institut für experimentelle Onkologie und Therapieforschung