2R4F
Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors
2R4F の概要
エントリーDOI | 10.2210/pdb2r4f/pdb |
関連するPDBエントリー | 2Q1L 2Q6B 2Q6C 3BGL |
分子名称 | 3-hydroxy-3-methylglutaryl-coenzyme A reductase, SULFATE ION, (3R,5R)-7-[1-(4-fluorophenyl)-4-(1-methylethyl)-3-{methyl[(1R)-1-phenylethyl]carbamoyl}-1H-pyrazol-5-yl]-3,5-dihydroxyheptanoic acid, ... (4 entities in total) |
機能のキーワード | oxidoreductase, cholesterol, biocynthesis, hmg-coa, nadph, statin, alternative splicing, cholesterol biosynthesis, endoplasmic reticulum, glycoprotein, lipid synthesis, membrane, peroxisome, polymorphism, steroid biosynthesis, sterol biosynthesis, transmembrane |
由来する生物種 | Homo sapiens (human) |
細胞内の位置 | Endoplasmic reticulum membrane; Multi-pass membrane protein: P04035 |
タンパク質・核酸の鎖数 | 4 |
化学式量合計 | 192404.90 |
構造登録者 | Pavlovsky, A.,Pfefferkorn, J.A.,Harris, M.S.,Finzel, B.C. (登録日: 2007-08-31, 公開日: 2008-04-29, 最終更新日: 2024-02-21) |
主引用文献 | Pfefferkorn, J.A.,Choi, C.,Larsen, S.D.,Auerbach, B.,Hutchings, R.,Park, W.,Askew, V.,Dillon, L.,Hanselman, J.C.,Lin, Z.,Lu, G.H.,Robertson, A.,Sekerke, C.,Harris, M.S.,Pavlovsky, A.,Bainbridge, G.,Caspers, N.,Kowala, M.,Tait, B.D. Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia. J.Med.Chem., 51:31-45, 2008 Cited by PubMed: 18072721DOI: 10.1021/jm070849r 主引用文献が同じPDBエントリー |
実験手法 | X-RAY DIFFRACTION (1.7 Å) |
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