4nrc

Crystal Structure of the bromodomain of human BAZ2B in complex with compound-3 N01186

spinqualitylabelsall models 4nrc, resolution 1.86Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4nrc is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.86Å Ligands: 15P, 2LY, EDO Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function BAZ2B_HUMAN May play a role in transcriptional regulation interacting with ISWI. Publication Abstract from PubMed Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain using biophysical fragment screening and structure-based optimization of high ligand-efficiency fragments into a novel series of low-micromolar inhibitors. Our results provide attractive leads for development of BAZ2B chemical probes and indicate the whole family may be tractable. Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.,Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz JR, Felletar I, von Delft F, Heightman T, Knapp S, Abell C, Ciulli A J Med Chem. 2013 Dec 27;56(24):10183-7. doi: 10.1021/jm401582c. Epub 2013 Dec 13. PMID:24304323 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Bromodomain adjacent to zinc finger 3D structures

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