WDR5-0103 is a selective antagonist of WD repeat-containing protein 5 (WDR5) with Kd of 450 nM.
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WDR5 (WD40 repeat protein 5) is an essential component of the human trithorax-like family of SET1 (Su(var)3-9 enhancer-of-zeste trithorax 1) methyltransferase complexes that carry out trimethylation of histone 3 Lys4 (H3K4me3), play key roles in development and are abnormally expressed in many cancers. WDR5-0103 is a potent and selective WDR5 antagonist with Kd of 450 nM. At an MLL (mixed-lineage leukaemia protein) complex concentration of 0.125 μM, WDR5-0103 inhibited MLL catalytic activity with an IC50 value of 39±10 μM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83±10 and 280±12 μM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data were consistent with a mechanism of action in which WDR5-0103 antagonized the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5[2].
作用机制
The methoxyphenyl and ester groups of WDR5-0103 increase shape complementarity with the binding pocket[2].
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