4TZ2

Fragment-Based Screening of the Bromodomain of ATAD2

Summary for 4TZ2

Entry DOI	10.2210/pdb4tz2/pdb
Related	4TYL 4TZ8
Descriptor	ATPase family AAA domain-containing protein 2, SULFATE ION, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... (6 entities in total)
Functional Keywords	atad2, bromodomain, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
Biological source	Homo sapiens (Human)
Total number of polymer chains	1
Total formula weight	15994.90
Authors	Harner, M.J.,Chauder, B.A.,Phan, J.,Fesik, S.W. (deposition date: 2014-07-09, release date: 2014-10-29, Last modification date: 2024-11-06)
Primary citation	Harner, M.J.,Chauder, B.A.,Phan, J.,Fesik, S.W. Fragment-Based Screening of the Bromodomain of ATAD2. J.Med.Chem., 57:9687-9692, 2014 Cited by PubMed 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. PubMed: 25314628 DOI: 10.1021/jm501035j PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.7 Å)

Structure validation