UNC4976 is a cell penetrant and potent positive allosteric modulator (PAM) of CBX7 chromodomain of polycomb repressive complex 1 that enhances CBX7 chromodomain affinity for nucleic acids. UNC4976 substantially potentiates the expression of polycomb target genes.
cell penetrant and potent positive allosteric modulator (PAM) of CBX7 chromodomain
Cell chemical biology, 26(10), 1365-1379 (2019-08-20)
Polycomb-directed repression of gene expression is frequently misregulated in human diseases. A quantitative and target-specific cellular assay was utilized to discover the first potent positive allosteric modulator (PAM) peptidomimetic, UNC4976, of nucleic acid binding by CBX7, a chromodomain methyl-lysine reader
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