Abstract
Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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ATPases Associated with Diverse Cellular Activities
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Adenosine Triphosphatases / chemistry*
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Antineoplastic Agents / chemistry
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Binding Sites
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray / methods
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DNA-Binding Proteins / chemistry*
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Humans
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Kinetics
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Ligands
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Magnetic Resonance Spectroscopy / methods
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Molecular Conformation
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Neoplasms / drug therapy
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Protein Structure, Tertiary
Substances
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Antineoplastic Agents
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DNA-Binding Proteins
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Ligands
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Adenosine Triphosphatases
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ATAD2 protein, human
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ATPases Associated with Diverse Cellular Activities