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WDR5 inhibitors and degraders act on WD repeat domain 5 (WDR5), a chromatin scaffold protein. WDR5 is a core subunit of the mixed-lineage leukemia (MLL) complexes that methylate lysine 4 of histone H3 (H3K4). A 2005 study showed that WDR5 binds methylated H3K4 and is required for this methylation and for vertebrate development. In 2015 WDR5 was also shown to help the transcription factor c-Myc recognize its target genes. OICR-9429, MM-589 and WDR5-0103 block the interaction between WDR5 and MLL. MS67 and MS33 are degraders that remove WDR5 protein from cells instead of only occupying a binding site.
