4tz2

Fragment-Based Screening of the Bromodomain of ATAD2

spinqualitylabelsall models 4tz2, resolution 1.70Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4tz2 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 39R, CL, SO4, TRS NonStd Res: CSO Related: 4tyl, 4tz8 Gene: ATAD2, L16, PRO2000 (HUMAN) Activity: Adenosinetriphosphatase, with EC number 3.6.1.3 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [ATAD2_HUMAN] May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells. Publication Abstract from PubMed 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. Fragment-based screening of the bromodomain of ATAD2.,Harner MJ, Chauder BA, Phan J, Fesik SW J Med Chem. 2014 Oct 14. PMID:25314628 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also ATPase family AAA domain-containing protein

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