Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3

[Image: see text] SMYD3 is a histone methyltransferase that regulates gene transcription, and its overexpression is associated with multiple human cancers. A novel class of tetrahydroacridine compounds which inhibit SMYD3 through a covalent mechanism of action is identified. Optimization of these ir...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: Huang, Chuhui, Liew, Si Si, Lin, Grace R., Poulsen, Anders, Ang, Melgious J. Y., Chia, Brian C. S., Chew, Sin Yin, Kwek, Zekui P., Wee, John L. K., Ong, Esther H., Retna, Priya, Baburajendran, Nithya, Li, Rong, Yu, Weixuan, Koh-Stenta, Xiaoying, Ngo, Anna, Manesh, Sravanthy, Fulwood, Justina, Ke, Zhiyuan, Chung, Hwa Hwa, Sepramaniam, Sugunavathi, Chew, Xin Hui, Dinie, Nurul, Lee, May Ann, Chew, Yun Shan, Low, Choon Bing, Pendharkar, Vishal, Manoharan, Vithya, Vuddagiri, Susmitha, Sangthongpitag, Kanda, Joy, Joma, Matter, Alex, Hill, Jeffrey, Keller, Thomas H., Foo, Klement
Format: Artigo
Language:Inglês
Published: American Chemical Society 2019
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6580565/
https://ncbi.nlm.nih.gov/pubmed/31223458
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00170
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