The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy

被引：30

作者：

Ao, Nannan ^{[1
]}

Chen, Qianping ^{[1
]}

Liu, Geng ^{[1
]}

机构：

[1] Soochow Univ, Med Coll, Sch Radiat Med & Protect, Collaborat Innovat Ctr Radiol Med Jiangsu Higher, Suzhou 215123, Peoples R China

来源：

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING | 2017年 / 20卷 / 05期

关键词：

Ubiquitin; cancer; small molecule inhibitors; proteasome; E3; ligase; deubiquitinating enzyme; LOW-DOSE DEXAMETHASONE; MULTIPLE-MYELOMA CELLS; IN-VITRO; DEUBIQUITINASE INHIBITION; UBC13-UEV1A INTERACTION; IRREVERSIBLE INHIBITOR; PRECLINICAL MODELS; ANTITUMOR-ACTIVITY; MDM2; INHIBITOR; 26S PROTEASOME;

D O I：

10.2174/1386207320666170710124746

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Background & Aim: The ubiquitin-proteasome system (UPS) is the major pathway for degrading the intracellular proteins. The 2004 Nobel Prize in Chemistry was awarded to Rose, Hershko, and Ciechanover to highlight the fundamental importance of UPS. Method & Results: The alterations in this process have been shown to contribute to the cancer progression. Hence, UPS has become a popular target for developing chemotherapeutics against tumours. The application of bortezomib showed high efficiency in treating haematological malignancies by interfering with UPS activity. Many compounds are being screened and evaluated in recent pharmacological advances, either as single agents or in synergy with other drugs, and more to be revealed. Conclusion: In the present review, we exhibit the crucial ingredients involved in UPS and discuss the current situation of small molecules targeting various components of ubiquitination pathway in cancer treatment.

引用

页码：403 / 413

页数：11

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