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  2. 上海药物研究所
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  4. 新药研究国家重点实验室
Discovery of new small molecule inhibitors of the BPTF bromodomain

文献类型：期刊论文

作者Liang, Xiaochen2,4,6; Cao, Yu4,5; Duan, Zhe4; Wang, Mingchen4; Zhang, Naixia4; Ding, Yiluan4; Luo, Cheng1,2,3,4,5; Lu, Na6; Chen, Shijie2,4
刊名BIOORGANIC CHEMISTRY
出版日期2023-05-01
卷号134页码:106453
关键词BPTF bromodomain BPTF inhibitors HTRF c-Myc
DOI10.1016/j.bioorg.2023.106453
文献子类Article
英文摘要Chromatin remodeling regulates many basic cellular processes, such as gene transcription, DNA repair, and programmed cell death. As the largest member of nucleosome remodeling factor (NURF), BPTF plays a vital role in the occurrence and development of cancer. Currently, BPTF bromodomain inhibitors are still in development. In this study, by conducting homogenous time-resolved fluorescence resonance energy transfer (HTRF) assay, we identified a potential, novel BPTF inhibitor scaffold Sanguinarine chloride with the IC50 value of 344.2 +/- 25.1 nM. Biochemical analysis revealed that compound Sanguinarine chloride exhibited high binding affinity to the BPTF bromodomain. Molecular docking predicted the binding mode of Sanguinarine chloride and elucidated the activities of its derivatives. Moreover, Sanguinarine chloride showed a potent anti-proliferative effect in MIAPaCa-2 cells and inhibited the expression of BPTF target gene c-Myc. Taken together, Sanguinarine chloride provides a qualified chemical tool for developing potent BPTF bromodomain inhibitors.
WOS关键词PROTEIN ; SANGUINARINE
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000954529700001
出版者ACADEMIC PRESS INC ELSEVIER SCIENCE
源URL[http://119.78.100.183/handle/2S10ELR8/309677]  
专题新药研究国家重点实验室
通讯作者Lu, Na; Chen, Shijie
作者单位1.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China;
3.Shanghai Tech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China;
4.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Chem Biol, State Key Lab Drug Res,Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China;
5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Jiangsu, Peoples R China;
6.China Pharmaceut Univ, Dept Physiol, State Key Lab Nat Med, Jiangsu Key Lab Carcinogenesis & Intervent,Sch Bas, Nanjing 210009, Peoples R China;
推荐引用方式
GB/T 7714		 Liang, Xiaochen,Cao, Yu,Duan, Zhe,et al. Discovery of new small molecule inhibitors of the BPTF bromodomain[J]. BIOORGANIC CHEMISTRY,2023,134:106453.
APA Liang, Xiaochen.,Cao, Yu.,Duan, Zhe.,Wang, Mingchen.,Zhang, Naixia.,...&Chen, Shijie.(2023).Discovery of new small molecule inhibitors of the BPTF bromodomain.BIOORGANIC CHEMISTRY,134,106453.
MLA Liang, Xiaochen,et al."Discovery of new small molecule inhibitors of the BPTF bromodomain".BIOORGANIC CHEMISTRY 134(2023):106453.

入库方式： OAI收割

来源：上海药物研究所

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