Fragment-based screening of the bromodomain of ATAD2.

Harner MJ, Chauder BA, Phan J, Fesik SW
J Med Chem. 2014 57 (22): 9687-92

PMID: 25314628 · PMCID: PMC4255743 · DOI:10.1021/jm501035j

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.

MeSH Terms (14)

Adenosine Triphosphatases Antineoplastic Agents ATPases Associated with Diverse Cellular Activities Binding Sites Chemistry, Pharmaceutical Crystallography, X-Ray DNA-Binding Proteins Humans Kinetics Ligands Magnetic Resonance Spectroscopy Molecular Conformation Neoplasms Protein Structure, Tertiary

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