Small-Molecule Inhibitors Targeting Protein Sumoylation As Novel Anticancer Compounds
1521-0111/94/2/885–894$35.00 https://doi.org/10.1124/mol.118.112300 MOLECULAR PHARMACOLOGY Mol Pharmacol 94:885–894, August 2018 Copyright ª 2018 by The American Society for Pharmacology and Experimental Therapeutics MINIREVIEW Small-Molecule Inhibitors Targeting Protein SUMOylation as Novel Anticancer Compounds Yanfang Yang, Zijing Xia, Xixi Wang, Xinyu Zhao, Zenghua Sheng, Yang Ye, Gu He, Liangxue Zhou, Hongxia Zhu, Ningzhi Xu, and Shufang Liang State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Downloaded from Center for Biotherapy, Chengdu (Y.Ya., Z.X., X.W., X.Z., Z.S., Y.Ye., G.H., L.Z., N.X., S.L.); Departments of Nephrology (Z.X.) and Neurosurgery (L.Z.), West China Hospital, Sichuan University, Chengdu; and Laboratory of Cell and Molecular Biology, and State Key Laboratory of Molecular Oncology, Cancer Institute and Cancer Hospital, Chinese Academy of Medical Sciences, Beijing (H.Z., N.X.), People’sRepublicofChina Received February 26, 2018; accepted May 16, 2018 molpharm.aspetjournals.org ABSTRACT SUMOylation, one of post-translational modifications, is co- biologic functions in cancer progression, numerous small- valently modified on lysine residues of a target protein through an molecule inhibitors targeting protein SUMOylation pathway are enzymatic cascade reaction similar to protein ubiquitination. developed as potentially clinical anticancer therapeutics. Here, Along with identification of many SUMOylated proteins, protein we systematically summarize the latest progresses of associa- SUMOylation has been proven to regulate multiple biologic tions of small ubiquitin-like modifier (SUMO) enzymes with activities including transcription, cell cycle, DNA repair, and cancers and small-molecular inhibitors against human cancers innate immunity.
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