2R4F
Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors
Summary for 2R4F
Entry DOI | 10.2210/pdb2r4f/pdb |
Related | 2Q1L 2Q6B 2Q6C 3BGL |
Descriptor | 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) |
Functional Keywords | oxidoreductase, cholesterol, biocynthesis, hmg-coa, nadph, statin, alternative splicing, cholesterol biosynthesis, endoplasmic reticulum, glycoprotein, lipid synthesis, membrane, peroxisome, polymorphism, steroid biosynthesis, sterol biosynthesis, transmembrane |
Biological source | Homo sapiens (human) |
Cellular location | Endoplasmic reticulum membrane; Multi-pass membrane protein: P04035 |
Total number of polymer chains | 4 |
Total formula weight | 192404.90 |
Authors | Pavlovsky, A.,Pfefferkorn, J.A.,Harris, M.S.,Finzel, B.C. (deposition date: 2007-08-31, release date: 2008-04-29, Last modification date: 2024-02-21) |
Primary citation | 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 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.7 Å) |
Structure validation
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