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PDBe Entry: 2r4f 
Substituted Pyrazoles as Hepatselective HMG-COA reductase inhibitors
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OXIDOREDUCTASE
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X-RAY DIFFRACTION
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Resolution: 1.7 Å, R-factor: 21.5%, Free R-factor: 23.4%, Spacegroup: P 1 21 1
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29/04/2008, deposition: 31/08/2007, last revision: 24/02/2009
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Pavlovsky, A.; Pfefferkorn, J.A.; Harris, M.S.; Finzel, B.C.
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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. vol:51, pag:31-45 (2008) [PubMed ID 18072721 ]
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OXIDOREDUCTASE, CHOLESTEROL, BIOCYNTHESIS, HMG-COA, NADPH, STATIN, Alternative splicing, Cholesterol biosynthesis, Endoplasmic reticulum, Glycoprotein, Lipid synthesis, Membrane, Peroxisome, Polymorphism, Steroid biosynthesis, Sterol biosynthesis, Transmembrane
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1.1.1.34 ExPASy BRENDA (A B C D)
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Homo sapiens(human) 9606(A B C D)
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3-hydroxy-3-methylglutaryl-coenzyme A reductase (EC 1.1.1.34) (HMG-CoA reductase) P04035 (A B C D)
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A, B, C, D
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2q1l, 2q6b, 2q6c, 3bgl
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| A, B, C, D |
3-hydroxy-3-methylglutaryl-coenzyme A reductase |
Protein |
P04035 (HMDH_HUMAN)
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441 |
95% |
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| A, B, C, D |
SULFATE ION |
SO4
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| A, B, C, D |
(3R,5R)-7-[1-(4-FLUOROPHENYL)-4-(1-METHYLETHYL)-3-{METHYL[(1R)-1-PHENYLETHYL]CARBAMOYL}-1H-PYRAZOL-5-YL]-3,5-DIHYDROXYHEPTANOIC ACID |
RIE
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