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  • Title: Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).
    Author: Korosec T, Acimovic J, Seliskar M, Kocjan D, Tacer KF, Rozman D, Urleb U.
    Journal: Bioorg Med Chem; 2008 Jan 01; 16(1):209-21. PubMed ID: 17964172.
    Abstract:
    Novel cholesterol biosynthesis inhibitors, a group of pyridylethanol(phenylethyl)amine derivatives, were synthesized. Sterol profiling assay in the human hepatoma HepG2 cells revealed that compounds target human lanosterol 14alpha-demethylase (CYP51). Structure-activity relationship study of the binding with the overexpressed human CYP51 indicates that the pyridine binds within the heme binding pocket in an analogy with the azoles.
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