Fragment-Based Screening of the Bromodomain of ATAD2

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 crysta...

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Veröffentlicht in:	Journal of medicinal chemistry 2014-11, Vol.57 (22), p.9687-9692
Hauptverfasser:	Harner, Mary J, Chauder, Brian A, Phan, Jason, Fesik, Stephen W
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Adenosine Triphosphatases - chemistry Antineoplastic Agents - chemistry ATPases Associated with Diverse Cellular Activities BASIC BIOLOGICAL SCIENCES Binding Sites Brief Chemistry, Pharmaceutical - methods Crystallography, X-Ray - methods DNA-Binding Proteins - chemistry Humans Kinetics Ligands Magnetic Resonance Spectroscopy - methods Molecular Conformation Neoplasms - drug therapy Protein Structure, Tertiary
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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm501035j