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Literature summary for 1.1.1.34 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

Application Comment Organism
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

Inhibitors Comment Organism Structure
atorvastatin
-
Homo sapiens
cerivastatin
-
Homo sapiens
fluvastatin
-
Homo sapiens
pravastatin
-
Homo sapiens
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
simvastatin
-
Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein
-
Homo sapiens

Reaction

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

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

Ki Value [mM]

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