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Title:

Systematic comparison of peptidic proteasome inhibitors highlights the ?-ketoamide electrophile as an auspicious reversible lead motif.

Document type:
Journal Article; Research Support, Non-U.S. Gov't; Article
Author(s):
Stein, Martin L; Cui, Haissi; Beck, Philipp; Dubiella, Christian; Voss, Constantin; Krüger, Achim; Schmidt, Boris; Groll, Michael
Abstract:
The ubiquitin-proteasome system (UPS) has been successfully targeted by both academia and the pharmaceutical industry for oncological and immunological applications. Typical proteasome inhibitors are based on a peptidic backbone endowed with an electrophilic C-terminus by which they react with the active proteolytic sites. Although the peptide moiety has attracted much attention in terms of subunit selectivity, the target specificity and biological stability of the compounds are largely determin...     »
Journal title abbreviation:
Angew Chem Int Ed Engl
Year:
2014
Journal volume:
53
Journal issue:
6
Pages contribution:
1679-83
Language:
eng
Fulltext / DOI:
doi:10.1002/anie.201308984
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/24403024
Print-ISSN:
1433-7851
TUM Institution:
Institut für Experimentelle Onkologie und Therapieforschung
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