Antagonist of chromodomains CBX4/7 of Polycomb repressive complex 1
UNC3866 inhibits the CBX chromodomains of the Polycomb repressive complex 1 (PRC1), which is involved in transcriptional repression. UNC3866 selectively targets CBX4 and CBX7 most potently, with Kd values of ∼100 nM. The PRC1 chromodomains facilitate PRC1-mediated transcriptional repression by targeting the complex to Trimethyllysine 27 on histone 3 (H3K27me3). UNC3866 antagonizes the methyllysine (Kme) reading function, and has been shown to inhibit the PC3 prostate cancer cell proliferation associated with CBX7 overexpression.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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Not applicable
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Not applicable
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Nature chemical biology, 12(3), 180-187 (2016-01-26)
We report the design and characterization of UNC3866, a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. Polycomb CBX proteins regulate gene expression by targeting Polycomb repressive complex 1 (PRC1) to
