P3 and P4 position analysis of vinyl ester pseudopeptide proteasome inhibitors

被引：19

作者：

Marastoni, Mauro ^{[1
]}

Baldisserotto, Anna

Trapella, Claudio

Gavioli, Riccardo

Tomatis, Roberto

机构：

[1] Univ Ferrara, Dept Pharmaceut Sci, 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：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 12期

关键词：

proteasome inhibitors; trypsin-like activity; solid-phase synthesis; small libraries;

D O I：

10.1016/j.bmcl.2006.03.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two small libraries of tripeptidic-based vinyl ester derivative proteasome inhibitors were synthesized and tested, starting with the Hmb-Val-Gln-Leu-VE prototype. The P3 and P4 positions were investigated with a complete set of amino acid residues, some of which showed remarkable selective inhibition of the trypsin-like (beta 2)subunit. In both positions, aromatic and hydrophobic residues were preferred. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3125 / 3130

页数：6

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