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Article

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors

9 Jul 2015

Abstract excerpt

Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of these effects upon the ATAD2 bromodomain, which has been categorized as among the least tractable of its class. The absence of any potent, selective inhibitors...

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PMID: 26155854
DOI: 10.1021/acs.jmedchem.5b00772

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