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Literature summary extracted from

  • Holdgate, G.A.; Ward, W.H.; McTaggart, F.
    Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin (2003), Biochem. Soc. Trans., 31, 528-531.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.1.1.34 medicine the enzyme is a target for intervention in the treatment of hypercholesterolaemia, clinical utility of inhibitors to decrease the levels of atherogenic lipiproteins in patients Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.34 atorvastatin
-
 Homo sapiens
1.1.1.34 cerivastatin
-
 Homo sapiens
1.1.1.34 fluvastatin
-
 Homo sapiens
1.1.1.34 pravastatin
-
 Homo sapiens
1.1.1.34 rosuvastatin thermodynamics of binding and inhibition mechanism, Glu559 is involved, reversible, 2-step complex formation, competitive with respect to 3-hydroxy-3-methylglutaryl-CoA, non-competitive to NADPH Homo sapiens
1.1.1.34 simvastatin
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.34 endoplasmic reticulum transmembrane protein Homo sapiens 5783
-
1.1.1.34 membrane transmembrane protein Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.34 (S)-3-hydroxy-3-methylglutaryl-CoA + NADPH + H+ Homo sapiens first step reaction mevaldyl-CoA + NADP+
-
 ?
1.1.1.34 mevaldyl-CoA + NADPH + H+ + H2O Homo sapiens second step reaction (R)-mevalonate + CoA + NADP+
-
 ?
1.1.1.34 additional information Homo sapiens the reaction is a highly regulated process within the cholesterol biosynthetic pathway ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.34 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
1.1.1.34 glycoprotein
-
 Homo sapiens

Reaction

EC Number Reaction Comment Organism Reaction ID
1.1.1.34 (R)-mevalonate + CoA + 2 NADP+ = (S)-3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+ Glu559 and His866 are involved in catalysis Homo sapiens
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.34 (S)-3-hydroxy-3-methylglutaryl-CoA + NADPH + H+ first step reaction Homo sapiens mevaldyl-CoA + NADP+
-
 ?
1.1.1.34 mevaldyl-CoA + NADPH + H+ + H2O second step reaction Homo sapiens (R)-mevalonate + CoA + NADP+
-
 ?
1.1.1.34 additional information the reaction is a highly regulated process within the cholesterol biosynthetic pathway Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.34 3-hydroxy-3-methylglutaryl CoA reductase
-
 Homo sapiens
1.1.1.34 HMG-CoAR
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.34 NADPH
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.34 additional information
-
 additional information steady state inhibition kinetics Homo sapiens
1.1.1.34 0.0000035
-
 rosuvastatin
-
 Homo sapiens
1.1.1.34 0.000008
-
 atorvastatin
-
 Homo sapiens
1.1.1.34 0.00001
-
 cerivastatin
-
 Homo sapiens
1.1.1.34 0.000011
-
 simvastatin
-
 Homo sapiens
1.1.1.34 0.000028
-
 fluvastatin
-
 Homo sapiens
1.1.1.34 0.000044
-
 pravastatin
-
 Homo sapiens