High-Resolution Snapshots of Proteasome Inhibitors in Action Revise Inhibition Paradigms and Inspire Next-Generation Inhibitor Design

被引：12

作者：

Carmony, Kimberly ^{[1
]}

Lee, Wooin ^{[2
,3
]}

Kim, Kyung Bo ^{[1
]}

机构：

[1] Univ Kentucky, Dept Pharmaceut Sci, 789 South Limestone St, Lexington, KY 40536 USA

[2] Seoul Natl Univ, Coll Pharm, 1 Gwanak Ro, Seoul 151742, South Korea

[3] Seoul Natl Univ, Pharmaceut Sci Res Inst, 1 Gwanak Ro, Seoul 151742, South Korea

来源：

CHEMBIOCHEM | 2016年 / 17卷 / 22期

基金：

美国国家卫生研究院; 新加坡国家研究基金会;

关键词：

drug design; epoxyketone; oprozomib; proteasome inhibitors; proteasome structures; CRYSTAL-STRUCTURE; 20S PROTEASOME; MECHANISM; COMPLEX; YEAST;

D O I：

10.1002/cbic.201600488

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The proteasome, which mediates the ubiquitin-dependent degradation of intracellular proteins, is well recognized as an important anticancer target (Figure 1). So far, three inhibitors of this multiprotease complex have received FDA approval for treating multiple myeloma: the peptide boronic acids bortezomib and ixazomib and the peptide epoxyketone carfilzomib.([1]) Several other proteasome inhibitors have entered clinical trials, including the peptide boronic acid delanzomib and the peptide epoxyketone oprozomib.([2]) [GRAPHICS] .

引用

页码：2115 / 2117

页数：3

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