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Article

A Box of Chemistry to Inhibit the MEN1 Tumor Suppressor Gene Promoting Leukemia

5 Feb 2021

Abstract excerpt

Targeting protein-protein interactions (PPIs) with small-molecule inhibitors has become a hotbed of modern drug development. In this review, we describe a new class of PPI inhibitors that block menin from binding to MLL proteins. Menin is encoded by the MEN1 tumor suppressor, but acts as an essential cofactor for MLL/KMT2A-rearranged leukemias. The most promising menin-MLL inhibitors belong to the...

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PMID: 33534953
DOI: 10.1002/cmdc.202000972

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