Abstract
ATAD2 (ANCCA) is an epigenetic regulator and transcriptional cofactor, whose overexpression has been linked to the progress of various cancer types. Here, we report a DNA-encoded library screen leading to the discovery of BAY-850, a potent and isoform selective inhibitor that specifically induces ATAD2 bromodomain dimerization and prevents interactions with acetylated histones in vitro, as well as with chromatin in cells. These features qualify BAY-850 as a chemical probe to explore ATAD2 biology.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATPases Associated with Diverse Cellular Activities / antagonists & inhibitors*
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ATPases Associated with Diverse Cellular Activities / chemistry
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ATPases Associated with Diverse Cellular Activities / metabolism*
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Cell Line, Tumor
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Chromatin / metabolism
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DNA-Binding Proteins / antagonists & inhibitors*
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DNA-Binding Proteins / chemistry
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DNA-Binding Proteins / metabolism*
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Drug Discovery
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Histones / metabolism
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Humans
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Ligands
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Models, Molecular
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Molecular Probes / chemistry*
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Molecular Probes / pharmacology*
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Protein Interaction Maps / drug effects*
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Protein Isoforms / antagonists & inhibitors
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Protein Isoforms / chemistry
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Protein Isoforms / metabolism
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Protein Multimerization / drug effects*
Substances
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Chromatin
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DNA-Binding Proteins
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Histones
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Ligands
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Molecular Probes
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Protein Isoforms
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ATAD2 protein, human
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ATPases Associated with Diverse Cellular Activities