Fragment-based screening of the bromodomain of ATAD2.
AUTHORS
Harner
MJMary J ,
Chauder
BABrian A ,
Phan
JJason ,
Fesik
SWStephen W .
Journal of medicinal chemistry. 2014 11 26; 57(22).
9687-92
- PMID: 25314628[PubMed].
- PMCID: PMC4255743.
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.