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Literature summary for 1.14.19.20 extracted from

  • Acimovic, J.; Korosec, T.; Seliskar, M.; Bjorkhem, I.; Monostory, K.; Szabo, P.; Pascussi, J.M.; Belic, A.; Urleb, U.; Kocjan, D.; Rozman, D.
    Inhibition of human sterol DELTA7-reductase and other postlanosterol enzymes by LK-980, a novel inhibitor of cholesterol synthesis (2011), Drug Metab. Dispos., 39, 39-46.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(4-phenethylpiperazin-1-yl)-1-(pyridine-3-yl)ethanol average content of 7-dehydrocholesterol in human primary hepatocytes after 2-(4-phenethylpiperazin-1-yl)-1-(pyridine-3-yl)ethanol treatment is, 34.16 times higher than that in nontreated cells, indicating that DHCR7 is the major target (minor targets are human sterol DELTA14-reductase, sterol DELTA24-reductase, and sterol C5-desaturase). In vitro kinetic measurements show that the half-life of 2-(4-phenethylpiperazin-1-yl)-1-(pyridine-3-yl)ethanol is at least 4.3 h. 2-(4-phenethylpiperazin-1-yl)-1-(pyridine-3-yl)ethanol does not induce CYP3A4 mRNA nor enzyme activity Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte primary hepatocytes are used for analysis Homo sapiens
-
liver
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
Dhcr7
-
Homo sapiens
sterol DELTA7-reductase
-
Homo sapiens