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Literature summary extracted from

  • Seiki, S.; Frishman, W.H.
    Pharmacologic inhibition of squalene synthase and other downstream enzymes of the cholesterol synthesis pathway: a new therapeutic approach to treatment of hypercholesterolemia (2009), Cardiol. Rev., 17, 70-76.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.14.14.17 drug development possible enzyme to inhibit for treatment of hypercholesterolemia, but strong side effects (e.g. dermatitis-like toxicity) Canis lupus familiaris
2.5.1.21 medicine aim of inhibitors in treatment of hypercholesterolemia Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.17 NB-598 decrease of LDL and triglyceride levels, dermatitis-like toxicity; decreases LDL and triglyceride levels, strong side effects (e.g. dermatitis-like toxicity) Canis lupus familiaris
1.14.14.17 NB-598 decrease of LDL and triglyceride levels, dermatitis-like toxicity Homo sapiens
1.14.14.17 NB-598 decrease of LDL and triglyceride levels, dermatitis-like toxicity Nicotiana sp.
2.5.1.21 BMS 187745 decrease of cholesterol or LDL Homo sapiens
2.5.1.21 BMS-188494 decrease of cholesterol or LDL Homo sapiens
2.5.1.21 BMS-188494 no induction of myotoxicity Rattus norvegicus
2.5.1.21 EP2302 decrease of cholesterol or LDL Homo sapiens
2.5.1.21 EP2302 decrease of cholesterol and triglyceride biosynthesis Oryctolagus cuniculus
2.5.1.21 EP2306 decrease of cholesterol or LDL Homo sapiens
2.5.1.21 EP2306 decrease of cholesterol and triglyceride biosynthesis Oryctolagus cuniculus
2.5.1.21 ER-27856 decrease of cholesterol biosynthesis Macaca sp.
2.5.1.21 ER-27856 decrease of cholesterol biosynthesis Rattus norvegicus
2.5.1.21 ER-28448 decrease of cholesterol biosynthesis Macaca sp.
2.5.1.21 ER-28448 decrease of cholesterol biosynthesis Rattus norvegicus
2.5.1.21 fenofibrate
-
 Cricetus cricetus
2.5.1.21 lapaquistat lipid-lowering effect Callithrix sp.
2.5.1.21 lapaquistat lipid-lowering effect Canis lupus familiaris
2.5.1.21 lapaquistat decrease of cholesterol or LDL Homo sapiens
2.5.1.21 lapaquistat lipid-lowering effect Macaca sp.
2.5.1.21 lapaquistat lipid-lowering effect Rattus norvegicus
2.5.1.21 RPR107393 reduction in plasma cholesterol concentrations Callithrix sp.
2.5.1.21 RPR107393 reduction of plasman cholesterol concentrations Rattus norvegicus
2.5.1.21 squalestatin hypolipidemic effects but potential toxicity because of high levels of urinary dicarboxylic acid Canis lupus familiaris
2.5.1.21 squalestatin hypolipidemic effects but potential toxicity because of high levels of urinary dicarboxylic acid Rattus norvegicus
2.5.1.21 YM-53601 decrease of non-high-density lipoprotein cholesterol Cavia porcellus
2.5.1.21 YM-53601 decrease of non-high-density lipoprotein cholesterol Cricetus cricetus
2.5.1.21 YM-53601 decrease of non-high-density lipoprotein cholesterol Macaca sp.
2.5.1.21 zaragozic acid hypolipidemic effects but potential toxicity because of high levels of urinary dicarboxylic acid Canis lupus familiaris
2.5.1.21 zaragozic acid hypolipidemic effects but potential toxicity because of high levels of urinary dicarboxylic acid Rattus norvegicus
5.4.99.7 U18666A produce cataract formation Metazoa

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.5.1.21 endoplasmic reticulum
-
 Cavia porcellus 5783
-
2.5.1.21 endoplasmic reticulum
-
 Mus musculus 5783
-
2.5.1.21 endoplasmic reticulum
-
 Homo sapiens 5783
-
2.5.1.21 endoplasmic reticulum
-
 Rattus norvegicus 5783
-
2.5.1.21 endoplasmic reticulum
-
 Oryctolagus cuniculus 5783
-
2.5.1.21 endoplasmic reticulum
-
 Canis lupus familiaris 5783
-
2.5.1.21 endoplasmic reticulum
-
 Callithrix sp. 5783
-
2.5.1.21 endoplasmic reticulum
-
 Cricetus cricetus 5783
-
2.5.1.21 endoplasmic reticulum
-
 Macaca sp. 5783
-
2.5.1.21 peroxisome
-
 Cavia porcellus 5777
-
2.5.1.21 peroxisome
-
 Mus musculus 5777
-
2.5.1.21 peroxisome
-
 Homo sapiens 5777
-
2.5.1.21 peroxisome
-
 Rattus norvegicus 5777
-
2.5.1.21 peroxisome
-
 Oryctolagus cuniculus 5777
-
2.5.1.21 peroxisome
-
 Canis lupus familiaris 5777
-
2.5.1.21 peroxisome
-
 Callithrix sp. 5777
-
2.5.1.21 peroxisome
-
 Cricetus cricetus 5777
-
2.5.1.21 peroxisome
-
 Macaca sp. 5777
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.21 Mg2+ cofactor Cavia porcellus
2.5.1.21 Mg2+ cofactor Mus musculus
2.5.1.21 Mg2+ cofactor Homo sapiens
2.5.1.21 Mg2+ cofactor Rattus norvegicus
2.5.1.21 Mg2+ cofactor Oryctolagus cuniculus
2.5.1.21 Mg2+ cofactor Canis lupus familiaris
2.5.1.21 Mg2+ cofactor Callithrix sp.
2.5.1.21 Mg2+ cofactor Cricetus cricetus
2.5.1.21 Mg2+ cofactor Macaca sp.

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.14.17 squalene + O2 + AH2 Homo sapiens
-
 2,3 oxidosqualene + A + H2O
-
 ?
1.14.14.17 squalene + O2 + AH2 Canis lupus familiaris
-
 2,3 oxidosqualene + A + H2O
-
 ?
1.14.14.17 squalene + O2 + AH2 Nicotiana sp.
-
 2,3 oxidosqualene + A + H2O
-
 ?
5.4.99.7 (S)-squalene-2,3-epoxide Metazoa
-
 Lanosterol
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.34 Homo sapiens
-
-
-
1.14.14.17 Canis lupus familiaris
-
-
-
1.14.14.17 Homo sapiens
-
-
-
1.14.14.17 Nicotiana sp.
-
-
-
2.5.1.21 Callithrix sp.
-
-
-
2.5.1.21 Canis lupus familiaris
-
-
-
2.5.1.21 Cavia porcellus
-
-
-
2.5.1.21 Cricetus cricetus
-
-
-
2.5.1.21 Homo sapiens
-
-
-
2.5.1.21 Macaca sp.
-
-
-
2.5.1.21 Mus musculus
-
-
-
2.5.1.21 Oryctolagus cuniculus
-
-
-
2.5.1.21 Rattus norvegicus
-
-
-
5.4.99.7 Metazoa
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.14.17 Hep-G2 cell
-
 Homo sapiens
-
1.14.14.17 myoblast
-
 Homo sapiens
-
2.5.1.21 hepatocyte
-
 Cavia porcellus
-
2.5.1.21 hepatocyte
-
 Mus musculus
-
2.5.1.21 hepatocyte
-
 Homo sapiens
-
2.5.1.21 hepatocyte
-
 Rattus norvegicus
-
2.5.1.21 hepatocyte
-
 Oryctolagus cuniculus
-
2.5.1.21 hepatocyte
-
 Canis lupus familiaris
-
2.5.1.21 hepatocyte
-
 Callithrix sp.
-
2.5.1.21 hepatocyte
-
 Cricetus cricetus
-
2.5.1.21 hepatocyte
-
 Macaca sp.
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.17 squalene + O2 + AH2
-
 Homo sapiens 2,3 oxidosqualene + A + H2O
-
 ?
1.14.14.17 squalene + O2 + AH2
-
 Canis lupus familiaris 2,3 oxidosqualene + A + H2O
-
 ?
1.14.14.17 squalene + O2 + AH2
-
 Nicotiana sp. 2,3 oxidosqualene + A + H2O
-
 ?
5.4.99.7 (S)-squalene-2,3-epoxide
-
 Metazoa Lanosterol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.34 3-hydroxymethylglutaryl coenzyme A reductase
-
 Homo sapiens
1.1.1.34 HMG-CoA reductase
-
 Homo sapiens
1.14.14.17 squalene epoxidase
-
 Homo sapiens
1.14.14.17 squalene epoxidase
-
 Canis lupus familiaris
1.14.14.17 squalene epoxidase
-
 Nicotiana sp.
2.5.1.21 squalene synthase
-
 Cavia porcellus
2.5.1.21 squalene synthase
-
 Mus musculus
2.5.1.21 squalene synthase
-
 Homo sapiens
2.5.1.21 squalene synthase
-
 Rattus norvegicus
2.5.1.21 squalene synthase
-
 Oryctolagus cuniculus
2.5.1.21 squalene synthase
-
 Canis lupus familiaris
2.5.1.21 squalene synthase
-
 Callithrix sp.
2.5.1.21 squalene synthase
-
 Cricetus cricetus
2.5.1.21 squalene synthase
-
 Macaca sp.
5.4.99.7 2,3 oxidosqualene:lanosterol cyclase
-
 Metazoa
5.4.99.7 Oxidosqualene cyclase
-
 Metazoa

Cofactor

EC Number Cofactor Comment Organism Structure
2.5.1.21 NADH
-
 Cavia porcellus
2.5.1.21 NADH
-
 Mus musculus
2.5.1.21 NADH
-
 Homo sapiens
2.5.1.21 NADH
-
 Rattus norvegicus
2.5.1.21 NADH
-
 Oryctolagus cuniculus
2.5.1.21 NADH
-
 Canis lupus familiaris
2.5.1.21 NADH
-
 Callithrix sp.
2.5.1.21 NADH
-
 Cricetus cricetus
2.5.1.21 NADH
-
 Macaca sp.
2.5.1.21 NADPH
-
 Cavia porcellus
2.5.1.21 NADPH
-
 Mus musculus
2.5.1.21 NADPH
-
 Homo sapiens
2.5.1.21 NADPH
-
 Rattus norvegicus
2.5.1.21 NADPH
-
 Oryctolagus cuniculus
2.5.1.21 NADPH
-
 Canis lupus familiaris
2.5.1.21 NADPH
-
 Callithrix sp.
2.5.1.21 NADPH
-
 Cricetus cricetus
2.5.1.21 NADPH
-
 Macaca sp.

General Information

EC Number General Information Comment Organism
1.1.1.34 metabolism part of cholesterol synthesis pathway Homo sapiens
1.14.14.17 metabolism part of cholesterol synthesis pathway Homo sapiens
1.14.14.17 metabolism part of cholesterol synthesis pathway Canis lupus familiaris
1.14.14.17 metabolism part of cholesterol synthesis pathway Nicotiana sp.
2.5.1.21 metabolism part of cholesterol synthesis pathway Cavia porcellus
2.5.1.21 metabolism part of cholesterol synthesis pathway Mus musculus
2.5.1.21 metabolism part of cholesterol synthesis pathway Homo sapiens
2.5.1.21 metabolism part of cholesterol synthesis pathway Rattus norvegicus
2.5.1.21 metabolism part of cholesterol synthesis pathway Oryctolagus cuniculus
2.5.1.21 metabolism part of cholesterol synthesis pathway Canis lupus familiaris
2.5.1.21 metabolism part of cholesterol synthesis pathway Callithrix sp.
2.5.1.21 metabolism part of cholesterol synthesis pathway Cricetus cricetus
2.5.1.21 metabolism part of cholesterol synthesis pathway Macaca sp.
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Cavia porcellus
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Mus musculus
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Rattus norvegicus
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Oryctolagus cuniculus
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Canis lupus familiaris
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Callithrix sp.
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Cricetus cricetus
2.5.1.21 physiological function influence on regulation of cholesterol metabolism Macaca sp.
5.4.99.7 metabolism part of cholesterol synthesis pathway Metazoa