Novel fluorinated pseudopeptides as proteasome inhibitors

被引：40

作者：

Formicola, Lucia ^{[1
]}

Marechal, Xavier ^{[2
]}

Basse, Nicolas ^{[2
]}

Bouvier-Durand, Michelle ^{[2
]}

Bonnet-Delpon, Daniele ^{[1
]}

Milcent, Thierry ^{[1
]}

Reboud-Ravaux, Michele ^{[2
]}

Ongeri, Sandrine ^{[1
]}

机构：

[1] Univ Paris 11, CNRS, UMR Mol Fluorees & Chim Med 8076, IFR 141,Fac Pharm, F-92296 Chatenay Malabry, France

[2] Univ Paris 06, FRE2852, CNRS, IJM, F-75251 Paris 05, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 01期

关键词：

Proteasome inhibitors; Pseudopeptide; Fluorine; Trifluoromethyl hydrazino; MEDICINAL CHEMISTRY; 20S PROTEASOME; DESIGN; PEPTIDOMIMETICS; BORTEZOMIB; PEPTIDE; ACCESS; ESTERS; DRUGS; CELLS;

D O I：

10.1016/j.bmcl.2008.11.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have designed novel small inhibitors of rabbit 20S proteasome using a trifluoromethyl-beta-hydrazino acid scaffold. Structural variations influenced their inhibition of the three types of active sites. Proteasome inhibition at the micromolar level was selective, calpain I and cathepsin B were not inhibited. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：83 / 86

页数：4

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