title: Fragment-based screening of the bromodomain of ATAD2.
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.
authors.affiliation: Department of Biochemistry, Vanderbilt University School of Medicine , 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
authors.forename: Mary J
authors.initials: MJ
authors.lastname: Harner
authors.forename: Brian A
authors.initials: BA
authors.lastname: Chauder
authors.forename: Jason
authors.initials: J
authors.lastname: Phan
authors.forename: Stephen W
authors.initials: SW
authors.lastname: Fesik
mesh_terms: D000074183:ATPases Associated with Diverse Cellular Activities; D000251:Adenosine Triphosphatases / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry; D001665:Binding Sites; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D004268:DNA-Binding Proteins / Q000737:chemistry*; D006801:Humans; D007700:Kinetics; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008968:Molecular Conformation; D009369:Neoplasms / Q000188:drug therapy; D017434:Protein Structure, Tertiary
chemical_list: D000970:Antineoplastic Agents; D004268:DNA-Binding Proteins; D008024:Ligands; D000251:Adenosine Triphosphatases; C544857:ATAD2 protein, human; D000074183:ATPases Associated with Diverse Cellular Activities