2wa4

FACTOR INHIBITING HIF-1 ALPHA WITH N,3-DIHYDROXYBENZAMIDEFACTOR INHIBITING HIF-1 ALPHA WITH N,3-DIHYDROXYBENZAMIDE

Structural highlights 2wa4 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: , , Related: 1mze, 2w0x, 2cgn, 1mzf, 1h2n, 1yci, 2wa3, 2cgo, 1h2k, 1iz3, 1h2m, 1h2l Activity: Peptide-aspartate beta-dioxygenase, with EC number 1.14.11.16 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Aromatic analogues of the 2-oxoglutarate co-substrate of the hypoxia-inducible factor hydroxylases are shown to bind at the active site iron: Pyridine-2,4-dicarboxylate binds as anticipated with a single molecule chelating the iron in a bidentate manner. The binding mode of a hydroxamic acid analogue, at least in the crystalline state, is unusual because two molecules of the inhibitor are observed at the active site and partial displacement of the iron binding aspartyl residue was observed. Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor.,Conejo-Garcia A, McDonough MA, Loenarz C, McNeill LA, Hewitson KS, Ge W, Lienard BM, Schofield CJ, Clifton IJ Bioorg Med Chem Lett. 2010 Oct 15;20(20):6125-8. Epub 2010 Aug 10. PMID:20822901 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Factor inhibiting HIF

spinqualitylabelsall models 2wa4, resolution 2.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image