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2R4F

Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors

Summary for 2R4F
Entry DOI10.2210/pdb2r4f/pdb
Related2Q1L 2Q6B 2Q6C 3BGL
Descriptor3-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 Keywordsoxidoreductase, cholesterol, biocynthesis, hmg-coa, nadph, statin, alternative splicing, cholesterol biosynthesis, endoplasmic reticulum, glycoprotein, lipid synthesis, membrane, peroxisome, polymorphism, steroid biosynthesis, sterol biosynthesis, transmembrane
Biological sourceHomo sapiens (human)
Cellular locationEndoplasmic reticulum membrane; Multi-pass membrane protein: P04035
Total number of polymer chains4
Total formula weight192404.90
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 citationPfefferkorn, 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: 18072721
DOI: 10.1021/jm070849r
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.7 Å)
Structure validation

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