The resistance mechanisms of proteasome inhibitor bortezomib

被引：139
作者：
Lü S. [1 ]
Wang J. [1 ]
机构：
[1] Department of Hematology, Changhai Hospital, Second Military Medical University, Shanghai 200433
来源：
Biomarker Research | / 1卷 / 1期
基金：
中国国家自然科学基金; 上海市自然科学基金;
关键词：
Bortezomib; Drug resistance; Mechanism; Proteasome inhibitor; PSMB5;
D O I：
10.1186/2050-7771-1-13
中图分类号：
学科分类号：
摘要：
The proteasome inhibitor, bortezomib, a boronic dipeptide which reversibly inhibit the chymotrypsin-like activity at the β5-subunit of proteasome (PSMB5), has marked efficacy against multiple myeloma and several non-Hodgkin's lymphoma subtypes, and has a potential therapeutic role against other malignancy diseases. However, intrinsic and acquired resistance to bortezomib may limit its efficacy. In this article, we discuss recent advances in the molecular understanding of bortezomib resistance. Resistance mechanisms discussed include mutations of PSMB5 and the up-regulation of proteasome subunits, alterations of gene and protein expression in stress response, cell survival and antiapoptotic pathways, and multidrug resistance. © 2013 Lü and Wang; licensee BioMed Central Ltd.
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