The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease

被引：35

作者：

Ontoria, JM ^{[1
]}

Di Marco, S ^{[1
]}

Conte, I ^{[1
]}

Di Francesco, ME ^{[1
]}

Gardelli, C ^{[1
]}

Koch, U ^{[1
]}

Matassa, VG ^{[1
]}

Poma, M ^{[1
]}

Steinkühler, C ^{[1
]}

Volpari, C ^{[1
]}

Harper, S ^{[1
]}

机构：

[1] IRBM, MRL, I-00040 Monte Porzio Catone, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 26期

关键词：

D O I：

10.1021/jm049435d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design of a series of peptidomimetic inhibitors of the hepatitis C virus NS3 protease is described. These inhibitors feature an indoline-2-carboxamide as a novel heterocyclic replacement for the P3 amino acid residue and N-terminal capping group of tripeptide based inhibitors. The crystal structure of the ternary NS3/NS4A/inhibitor complex for the most active molecule in this series highlights its suitability as an N-terminal capping group of a dipeptide inhibitor of the NS3 protease.

引用

页码：6443 / 6446

页数：4

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