2W0X
FACTOR INHIBITING HIF-1 ALPHA WITH PYRIDINE 2,4 DICARBOXYLIC ACID
Summary for 2W0X
| Entry DOI | 10.2210/pdb2w0x/pdb |
| Related | 1H2K 1H2L 1H2M 1H2N 1IZ3 1MZE 1MZF 1YCI 2CGN 2CGO 2WA3 2WA4 |
| Descriptor | HYPOXIA-INDUCIBLE FACTOR 1 ALPHA INHIBITOR, FE (II) ION, PYRIDINE-2,4-DICARBOXYLIC ACID, ... (6 entities in total) |
| Functional Keywords | hydroxylase, dioxygenase, transcription, oxidoreductase, transcription activator/inhibitor, hypoxia |
| Biological source | HOMO SAPIENS (HUMAN) |
| Cellular location | Nucleus: Q9NWT6 |
| Total number of polymer chains | 1 |
| Total formula weight | 40931.53 |
| Authors | Conejo-Garcia, A.,Lienard, B.M.R.,Clifton, I.J.,McDonough, M.A.,Schofield, C.J. (deposition date: 2008-10-10, release date: 2009-11-24, Last modification date: 2023-12-13) |
| Primary citation | Conejo-Garcia, A.,McDonough, M.A.,Loenarz, C.,McNeill, L.A.,Hewitson, K.S.,Ge, W.,Lienard, B.M.,Schofield, C.J.,Clifton, I.J. Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor. Bioorg. Med. Chem. Lett., 20:6125-6128, 2010 Cited by PubMed Abstract: 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. PubMed: 20822901DOI: 10.1016/j.bmcl.2010.08.032 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.12 Å) |
Structure validation
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