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

…, P Beck, C Dubiella, C Voss, A Krüger…

文献索引：Stein, Martin L.; Cui, Haissi; Beck, Philipp; Dubiella, Christian; Voss, Constantin; Krueger, Achim; Schmidt, Boris; Groll, Michael Angewandte Chemie - International Edition, 2014 , vol. 53, # 6 p. 1679 - 1683 Angew. Chem., 2014 , vol. 126, # 6 p. 1705 - 1709,5

全文：HTML全文

被引用次数: 32

摘要

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 ...