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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 15期

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

页码：5038 / 5042

页数：5

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