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5 results on '"Lian, Fulin"'

2. Data from A Small-Molecule Inhibitor Targeting TRIP13 Suppresses Multiple Myeloma Progression

Author

Wang, Yingcong, primary, Huang, Jing, primary, Li, Bo, primary, Xue, Han, primary, Tricot, Guido, primary, Hu, Liangning, primary, Xu, Zhijian, primary, Sun, Xiaoxiang, primary, Chang, Shuaikang, primary, Gao, Lu, primary, Tao, Yi, primary, Xu, Hongwei, primary, Xie, Yongsheng, primary, Xiao, Wenqin, primary, Yu, Dandan, primary, Kong, Yuanyuan, primary, Chen, Gege, primary, Sun, Xi, primary, Lian, Fulin, primary, Zhang, Naixia, primary, Wu, Xiaosong, primary, Mao, Zhiyong, primary, Zhan, Fenghuang, primary, Zhu, Weiliang, primary, and Shi, Jumei, primary

Published
2023
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3. Figure S1-S6, Table S1-S2 from A Small-Molecule Inhibitor Targeting TRIP13 Suppresses Multiple Myeloma Progression

Author

Wang, Yingcong, primary, Huang, Jing, primary, Li, Bo, primary, Xue, Han, primary, Tricot, Guido, primary, Hu, Liangning, primary, Xu, Zhijian, primary, Sun, Xiaoxiang, primary, Chang, Shuaikang, primary, Gao, Lu, primary, Tao, Yi, primary, Xu, Hongwei, primary, Xie, Yongsheng, primary, Xiao, Wenqin, primary, Yu, Dandan, primary, Kong, Yuanyuan, primary, Chen, Gege, primary, Sun, Xi, primary, Lian, Fulin, primary, Zhang, Naixia, primary, Wu, Xiaosong, primary, Mao, Zhiyong, primary, Zhan, Fenghuang, primary, Zhu, Weiliang, primary, and Shi, Jumei, primary

Published
2023
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5. Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation

Author

Wang, Chen, Jiang, Hao, Jin, Jia, Xie, Yiqian, Chen, Zhifeng, Zhang, Hao, Lian, Fulin, Liu, Yu-Chih, Zhang, Chenhua, Ding, Hong, Chen, Shijie, Zhang, Naixia, Zhang, Yuanyuan, Jiang, Hualiang, Chen, Kaixian, Ye, Fei, Yao, Zhiyi, and Luo, Cheng

Abstract

Protein Arginine Methyltransferases (PRMTs) are crucial players in diverse biological processes, and dysregulation of PRMTs has been linked to various human diseases, especially cancer. Therefore, small molecules targeting PRMTs have profound impact for both academic functional studies and clinical disease treatment. Here, we report the discovery of N1-(2-((2-chlorophenyl)thio)benzyl)-N1-methylethane-1,2-diamine (28d, DCPR049_12), a highly potent inhibitor of type I PRMTs that has good selectivity against a panel of other methyltransferases. Compound 28deffectively inhibits cell proliferation in several leukemia cell lines and reduces the cellular asymmetric arginine dimethylation levels. Serving as an effective inhibitor, 28ddemonstrates the mechanism of cell killing in both cell cycle arrest and apoptotic effect as well as downregulation of the pivotal mixed lineage leukemia (MLL) fusion target genes such as HOXA9and MEIS1, which reflects the critical roles of type I PRMTs in MLL leukemia. These studies present 28das a valuable inhibitor to investigate the role of type I PRMTs in cancer and other diseases.

Published
2024
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