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 | 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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
endoplasmic reticulum | transmembrane protein | Homo sapiens | 5783 | - |
membrane | transmembrane protein | Homo sapiens | 16020 | - |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
glycoprotein | - |
Homo sapiens |
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 | 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 | Comment | Organism |
---|---|---|
3-hydroxy-3-methylglutaryl CoA reductase | - |
Homo sapiens |
HMG-CoAR | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
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 |