Non-covalent inhibitors of the 20S proteasome

被引：1

作者：

García-Echeverría, C ^{[1
]}

Imbach, P ^{[1
]}

Roesel, J ^{[1
]}

Fuerst, P ^{[1
]}

Lang, M ^{[1
]}

Guagnano, V ^{[1
]}

Noorani, M ^{[1
]}

Zimmermann, J ^{[1
]}

Furet, P ^{[1
]}

机构：

[1] Novartis Pharma AG, Oncol Res, CH-4002 Basel, Switzerland

来源：

CHIMIA | 2003年 / 57卷 / 04期

关键词：

antitumor agents; drug design; enzyme inhibitors; peptidomimetic;

D O I：

10.2533/000942903777679415

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Peptidomimetics have been commonly used as lead compounds to design inhibitors with high affinity and specificity for a particular enzyme. The discovery that a 2-aminobenzylstatine derivative originally designed to target an aspartyl protease was able to inhibit specifically and non-covalently the chymotrypsin-like activity of the 20S proteasome represented a unique starting point for our medicinal chemistry endeavor for this target. Utilizing a structure-based design approach, we have been able to improve the potency of this new class of proteasome inhibitors without affecting its in vitro selectivity profile.

引用

页码：179 / 181

页数：3

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