Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14α-demethylase (CYP51)

Tina Korošec, Jure Ačimovič, Matej Seliškar, Darko Kocjan, Klementina Fon Tacer, Damjana Rozman, Uroš Urleb

Research output: Contribution to journalArticle

30 Scopus citations

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 14α-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.

Original languageEnglish (US)
Pages (from-to)209-221
Number of pages13
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number1
DOIs
Publication statusPublished - Jan 1 2008

    Fingerprint

Keywords

  • Cholesterol biosynthesis inhibitors
  • Cholesterol intermediates profile
  • Human lanosterol 14α-demethylase (CYP51) inhibitors
  • Pyridylethanolamines

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Korošec, T., Ačimovič, J., Seliškar, M., Kocjan, D., Tacer, K. F., Rozman, D., & Urleb, U. (2008). Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14α-demethylase (CYP51). Bioorganic and Medicinal Chemistry, 16(1), 209-221. https://doi.org/10.1016/j.bmc.2007.10.001