Fragment-Based Screening of the Bromodomain of ATAD2
Author(s) -
Mary J. Harner,
Brian A. Chauder,
Jason Phan,
Stephen W. Fesik
Publication year - 2014
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/jm501035j
Subject(s) - bromodomain , fragment (logic) , chemistry , nuclear magnetic resonance spectroscopy , small molecule , stereochemistry , computational biology , combinatorial chemistry , biochemistry , dna , algorithm , biology , computer science , histone
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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