Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 22, Pages 9687-9692Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm501035j
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Funding
- U.S. National Institutes of Health, NIH Director's Pioneer Award [DP1OD006933/DP1CA174419]
- Damon Runyon Cancer Research Foundation [DRG 2123-12]
- NSF [0922862]
- NIH [S10 RR025677]
- Vanderbilt University
- U.S. DOE [DE-AC02-06CH11357]
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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.
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