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Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein–Protein Interactions between DOT1L and MLL-AF9/MLL-ENL

25 May 2022

Abstract excerpt

On the basis of a previously identified DOT1L peptide mimetic (compound 3 ), a series of novel peptide mimetics were designed and synthesized. These compounds can potently bind to AF9 and ENL either in cell-free binding assays or in leukemia cells, and selectively inhibit the growth of leukemia cells containing mixed lineage leukemia (MLL) fusion proteins. The most potent compound 12 exhibited comparable...

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PMID: 35612819
DOI: 10.1021/acs.jmedchem.2c00083

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