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Novel cholesterol biosynthesis inhibitors targeting the human lanosterol 14[alpha]-demethylase (CYP51)
Korošec, Tina, 1976- ...
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 14[alpha]-demethylase (CYP51). Structure-activity relationship study of the binding with the overexpressed human CYP51 indicatesthat the pyridine binds within the heme binding pocket in an analogy with the azoles.
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