Citation: Hacer Karatas, Shirley Y. Lee, Elizabeth C. Townsend, Fang Cao, Jing Xu, Denzil Bernard, Liu Liu, Yali Dou, Shaomeng Wang. Structure-based design of conformationally constrained cyclic peptidomimetics to target the MLL1-WDR5 protein-protein interaction as inhibitors of the MLL1 methyltransferase activity[J]. Chinese Chemical Letters, ;2015, 26(4): 455-458. doi: 10.1016/j.cclet.2015.03.030
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We described herein structure-based design, synthesis and evaluation of conformationally constrained, cyclic peptidomimetics to block the MLL1-WDR5 protein-protein interaction as inhibitors of the MLL1 histone methyltransferase activity. Our study has yielded cyclic peptidomimetics with very high binding affinities to WDR5 (Ki values <1 nmol/L) and function as antagonists of the MLL1 histone methyltransferase activity.
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