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个人信息Personal Information
教授
博士生导师
硕士生导师
性别:男
毕业院校:大连理工大学
学位:博士
所在单位:生物工程学院
学科:生物化工. 生物工程与技术
联系方式:zhlxiu@dlut.edu.cn
电子邮箱:zhlxiu@dlut.edu.cn
基于Chlamydocin骨架设计合成环肽类HDACi及其抗肿瘤活性
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发表时间:2022-10-10
发表刊物:有机化学
所属单位:生物工程学院
卷号:31
期号:3
页面范围:312-316
ISSN号:0253-2786
摘要:Histone deacetylases (HDACs) profoundly affect cellular function by catalyzing removal of acetyl groups from N-acetylated lysine residues of various protein substrates including histones, transcription factors, alpha-tubulin, and nuclear importers. Inhibition of HDAC activity has emerged as a promising approach for reversing the aberrant epigenetic states associated with cancer and other chronic diseases. To know the structure-activity relationship cyclic peptide HDACi with HDACs, several novel HDACis with similar cyclic tetrapeptide framework as chlamydocin were designed and synthesized. The binding functional group was protected as disulfide. The macrocyclic frameworks were modified by introducing methyl at different sites of benzene ring of phenylalanine. HDACi was tested for cytotoxic activity against three cancer cell lines, including MCF-7, Hela and 7721 cells. All the compounds demonstrated exciting antitumor abilities, and were most active against Hela with IC(50) at 0.1 mu mol/L. The cellular shapes changed obviously, when the cells treated by HDACi.
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