Inhibition of the Human Proteasome by Imidazoline Scaffolds

被引：37

作者：

Azevedo, Lauren M. ^{[1
]}

Lansdell, Theresa A. ^{[1
]}

Ludwig, Jacob R. ^{[1
]}

Mosey, Robert A. ^{[1
]}

Woloch, Daljinder K. ^{[1
]}

Cogan, Dillon P. ^{[1
]}

Patten, Gregory P. ^{[1
]}

Kuszpit, Michael R. ^{[1
]}

Fisk, Jason S. ^{[1
]}

Tepe, Jetze J. ^{[1
]}

机构：

[1] Michigan State Univ, Dept Chem, E Lansing, MI 48824 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 56卷 / 14期

基金：

美国国家卫生研究院;

关键词：

BORTEZOMIB RESISTANCE; ALLOSTERIC MODULATORS; 20S PROTEASOME; ARMY;

D O I：

10.1021/jm400235r

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The proteasome has emerged as the primary target for the treatment of multiple myeloma. Unfortunately, nearly all patients develop resistance to competitive-type proteasome inhibitors such as bortezomib. Herein, we describe the optimization of noncompetitive proteasome inhibitors to yield derivatives that exhibit nanomolar potency (compound 49, IC50 130 nM) toward proteasome inhibition and overcome bortezomib resistance. These studies illustrate the feasibility of the development of noncompetitive proteasome inhibitors as additives and/or alternatives to competitive proteasome inhibitors.

引用

页码：5974 / 5978

页数：5

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