Win6mer is a potent and specific inhibitor of MLL1 and SETd1A histone H3 lysine 4 (H3K4) methyltransferase complexes that does not inhibit MLL2-4 or SETd1B complexes. Win6mer potently binds to WDR5 in a 310-helical conformation. It does not inhibit isolated SET domain activity.
potent and specific inhibitor of MLL1 and SETd1A histone H3 lysine 4 (H3K4) methyltransferase complexes
The Journal of biological chemistry, 291(43), 22357-22372 (2016-08-27)
MLL1 belongs to the SET1 family of histone H3 lysine 4 (H3K4) methyltransferases, composed of MLL1-4 and SETd1A/B. MLL1 translocations are present in acute leukemias, and mutations in several family members are associated with cancer and developmental disorders. MLL1 associates
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