Fragment-based screening of the bromodomain of ATAD2.

Authors

Harner MJ Mary J , Chauder BA Brian A , Phan J Jason , Fesik SW Stephen W .
Journal of medicinal chemistry. 2014 11 26; 57(22).
9687-92

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.