Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51) |
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Authors: | Korosec Tina Acimovic Jure Seliskar Matej Kocjan Darko Tacer Klementina Fon Rozman Damjana Urleb Uros |
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Institution: | Lek Pharmaceuticals d. d., Drug Discovery, 1000 Ljubljana, Verovskova 57, Slovenia. |
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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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