4TZ8

Structure of human ATAD2 bromodomain bound to fragment inhibitor

Summary for 4TZ8

Entry DOI	10.2210/pdb4tz8/pdb
Related	4TYL 4TZ2
Descriptor	ATPase family AAA domain-containing protein 2, SULFATE ION, CHLORIDE ION, ... (5 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	15892.38
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: 2023-09-27)
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 (2.15 Å)

Structure validation