Screening of human cytochrome P450(51) (CYP51A1) inhibitors: Structural lanosterol analogues of plant and animal origin

L. A. Kaluzhskiy, O. V. Gnedenko, A. A. Gilep, N. V. Strushkevich, T. V. Shkel, M. A. Chernovetsky, A. S. Ivanov, A. V. Lisitsa, A. S. Usanov, V. A. Stonik, A. I. Archakov

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

Abstract

Inhibition of cholesterol biosynthesis at post-squalene steps provide the alternative to classic statin therapy. Sterol-14α-demethylase (CYP51) is one of potential targets for such inhibition. In this study screening of potential ligands of human CYP51 (CYP51A1) among natural low-weight compounds containing steroid-like moiety has been performed by means of integration of surface plasmon resonance and spectral titration methods. Four compounds (betulafolientriol, holothurin A, theasaponin, capsicosine) exhibited high affinity to the active site of CYP51A1. These data extend the known range of compounds, which may be used as specific inhibitors of CYP51.

Original languageEnglish
Pages (from-to)349-360
Number of pages12
JournalBiochemistry (Moscow) Supplement Series B: Biomedical Chemistry
Volume8
Issue number4
DOIs
Publication statusPublished - 22 Nov 2014
Externally publishedYes

Keywords

  • CYP51
  • cytochrome P450
  • optical biosensor
  • spectral titration
  • surface plasmon resonance
  • triterpenes

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