Peptidyl vinyl ester derivatives: New class of selective inhibitors of proteasome trypsin-like activity

被引:34
|
作者
Marastoni, M
Baldisserotto, A
Cellini, S
Gavioli, R
Tomatis, R
机构
[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy
[2] Univ Ferrara, Ctr Biotechnol, I-44100 Ferrara, Italy
[3] Univ Ferrara, Dept Biochem & Mol Biol, I-44100 Ferrara, Italy
关键词
D O I
10.1021/JM040905D
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The proteasome is a multicatalytic proteinase complex which plays a central role in intracellular protein degradation. We report here the synthesis and biological activities of a new class of specific proteasome inhibitors selective for trypsin-like activity. These tripeptide-based compounds bearing a C-terminal vinyl ester are nontoxic, and do not affect cell proliferation, but are able to modulate the generation and presentation of immunogenic peptides presented by MHC class I molecules.
引用
收藏
页码:5038 / 5042
页数:5
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