Drug intelligence / Profile preview

Chinese Academy of Sciences EZH2 compound 38

Development stage
Unknown
Lead developer
Chinese Academy of Sciences
01

Overview

Chinese Academy of Sciences EZH2 compound 38: sourced facts only. name: "Starting from an approved EZH2 inhibitor EPZ-6438, we used covalent drug design and medicinal chemistry approaches to discover a novel covalent EZH2 degrader 38, which forms a covalent bond with EZH2 Cys663 and showed strong biochemical activities against EZH2 WT and mutants." [PMID:37826933]; target: "Starting from an approved EZH2 inhibitor EPZ-6438, we used covalent drug design and medicinal chemistry approaches to discover a novel covalent EZH2 degrader 38, which forms a covalent bond with EZH2 Cys663 and showed strong biochemical activities against EZH2 WT and mutants." [PMID:37826933]; developer: "Anhui Province Key Laboratory of Medical Physics and Technology, Institute of Health and Medical Technology, Hefei Institutes of Physical Science, Chinese Academy of Sciences, Hefei, Anhui, 230031, PR China; University of Science and Technology of China, Hefei, Anhui, 230026, PR China." [PMID:37826933]; stage: "Compound 38 exhibited potent antiproliferation effects against both B-cell lymphoma and TNBC cell lines by reducing the levels of H3K27me3 and EZH2." [PMID:37826933]

02

Targets

EZH2 (Histone-lysine N-methyltransferase EZH2)

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