5d7x | pdb_00005d7x

Crystal structure of the human BRPF1 bromodomain in complex with XZ08

spinqualitylabelsall models 5d7x, resolution 1.35Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5d7x 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. Ligands: NO3, XZ8 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function BRPF1_HUMAN Component of the MOZ/MORF complex which has a histone H3 acetyltransferase activity. Positively regulates the transcription of RUNX1 and RUNX2. Publication Abstract from PubMed Small-molecule hits for the bromodomains of CREBBP and BAZ2B have been identified by scaffold hopping followed by docking of a set of approximately 200 compounds containing the acetyl indole scaffold. Chemical synthesis of nearly 30 derivatives has resulted in ligands of representatives of three subfamilies of human bromodomains with favorable ligand efficiency. The X-ray crystal structures of three different bromodomains (CREBBP, BAZ2B, and BRPF1b) in complex with acetyl indole derivatives reveal the influence of the gatekeeper residue on the orientation of small-molecule ligands in the acetyl lysine binding site. The "Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.,Unzue A, Zhao H, Lolli G, Dong J, Zhu J, Zechner M, Dolbois A, Caflisch A, Nevado C J Med Chem. 2016 Apr 14;59(7):3087-97. doi: 10.1021/acs.jmedchem.5b01757. Epub, 2016 Mar 30. PMID:26982797 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

Proteopedia Page Contributors and Editors (what is this?)

OCA