[SPR-biosensor assay for analysis of small compounds interaction with human cytochrome P450 51A1 (CYP51A1)]

O V Gnedenko; L A Kaluzhskiĭ; A A Mol'nar; A V Iantsevich; D V Mukha; A A Gilep; S A Usanov; V A Stonik; A S Ivanov; A V Lisitsa; A I Archakov

doi:10.18097/pbmc20135904388

[SPR-biosensor assay for analysis of small compounds interaction with human cytochrome P450 51A1 (CYP51A1)]

Biomed Khim. 2013 Jul-Aug;59(4):388-98. doi: 10.18097/pbmc20135904388.

[Article in Russian]

Authors

O V Gnedenko, L A Kaluzhskiĭ, A A Mol'nar, A V Iantsevich, D V Mukha, A A Gilep, S A Usanov, V A Stonik, A S Ivanov, A V Lisitsa, A I Archakov

PMID: 24502137
DOI: 10.18097/pbmc20135904388

Abstract

The SPR assay for human cytochrome P450 51A1's (CYP51A1) ligand screening was developed. Assay has been validated with known azole inhibitors of cytochrome P450s. The studied azoles selectively interacted with human cytochrome P450 51A1, which showed the highest affinity towards ketoconazole. The efficiency of the SPR assay was showed with 19 steroid and triterpene compounds, which were not investigated as potential ligands of CYP51A1.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

14-alpha Demethylase Inhibitors / chemistry*
14-alpha Demethylase Inhibitors / metabolism
Biosensing Techniques*
Humans
Ketoconazole / chemistry*
Ketoconazole / metabolism
Protein Binding
Sterol 14-Demethylase / chemistry*
Sterol 14-Demethylase / metabolism

Substances

14-alpha Demethylase Inhibitors
CYP51A1 protein, human
Sterol 14-Demethylase
Ketoconazole