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Titel:

Selective inhibition of the immunoproteasome by ligand-induced crosslinking of the active site.

Dokumenttyp:
Journal Article; Research Support, Non-U.S. Gov't; Article
Autor(en):
Dubiella, Christian; Cui, Haissi; Gersch, Malte; Brouwer, Arwin J; Sieber, Stephan A; Krüger, Achim; Liskamp, Rob M J; Groll, Michael
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...     »
Zeitschriftentitel:
Angew Chem Int Ed Engl
Jahr:
2014
Band / Volume:
53
Heft / Issue:
44
Seitenangaben Beitrag:
11969-73
Sprache:
eng
Volltext / DOI:
doi:10.1002/anie.201406964
PubMed:
http://view.ncbi.nlm.nih.gov/pubmed/25244435
Print-ISSN:
1433-7851
TUM Einrichtung:
Institut für Experimentelle Onkologie und Therapieforschung
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