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

Gnedenko O.V.1 , Kaluzhskiy L.A.1, Molnar A.A.1, Yantsevich A.V.2, Mukha D.V.2, Gilep A.A.2, Usanov S.A.2, Stonik V.A.3, Ivanov A.S.1, Lisitsa A.V.1, Archakov A.I.1

1. Orekhovich Institute of Biomedical Chemistry of Russian Academy of Medical Sciences
2. Institute of Bioorganic Chemistry NASB
3. Pacific Institute of Bioorganic Chemistry, Far East Branch of Russian Academy of Sciences
Section: Experimental/Clinical Study
DOI: 10.18097/pbmc20135904388      UDK: 577.152.3      PubMed Id: 24502137
Year: 2013  Volume: 59  Issue: 4  Pages: 388-398
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.
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Gnedenko O.V., Kaluzhskiy L.A., Molnar A.A., Yantsevich A.V., Mukha D.V., Gilep A.A., Usanov S.A., Stonik V.A., Ivanov A.S., Lisitsa A.V., Archakov A.I. (2013) Biomeditsinskaya khimiya, 59(4), 388-398.
This paper is also available as the English translation:10.1134/S1990750813030049
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