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Small-Molecule Inhibitors Targeting Protein SUMOylation as Novel Anticancer Compounds.

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机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu [2]Departments of Nephrology,West China Hospital, Sichuan University, Chengdu [3]Departments of Neurosurgery,West China Hospital, Sichuan University, Chengdu [4]Laboratory of Cell and Molecular Biology, and State Key Laboratory of Molecular Oncology, Cancer Institute and Cancer Hospital, Chinese Academy of Medical Sciences, Beijing, People’s Republic of China
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SUMOylation, one of post-translational modifications, is covalently modified on lysine residues of a target protein through an enzymatic cascade reaction similar to protein ubiquitination. Along with identification of many SUMOylated proteins, protein SUMOylation has been proven to regulate multiple biologic activities including transcription, cell cycle, DNA repair, and innate immunity. The dysregulation of protein SUMOylation and deSUMOylation modification is linked with carcinogenesis and tumor progression. The SUMOylation-associated enzymes are usually elevated in various cancers, which function as cancer biomarkers to relate to poor outcomes for patients. Considering the significance of protein SUMOylation in regulating diverse biologic functions in cancer progression, numerous small-molecule inhibitors targeting protein SUMOylation pathway are developed as potentially clinical anticancer therapeutics. Here, we systematically summarize the latest progresses of associations of small ubiquitin-like modifier (SUMO) enzymes with cancers and small-molecular inhibitors against human cancers by targeting SUMOylation enzymes. We also compared the pros and cons of several special anticancer inhibitors targeting SUMO pathway. As more efforts are invested in this field, small-molecule inhibitors targeting the SUMOylation modification pathway are promising for development into novel anticancer drugs. Copyright © 2018 by The American Society for Pharmacology and Experimental Therapeutics.

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出版当年[2018]版:
大类 | 2 区 医学
小类 | 2 区 药学
最新[2023]版:
大类 | 3 区 医学
小类 | 3 区 药学
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出版当年[2018]版:
Q1 PHARMACOLOGY & PHARMACY
最新[2023]版:
Q2 PHARMACOLOGY & PHARMACY

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第一作者机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu
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通讯机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu [*1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, No. 17, 3rd Section of People’s South Road, Chengdu, 610041, People’s Republic of China.
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