The SPR-based biosensor test system for analysis of small compounds interaction with human cytochrome P450 51A1 (CYP51A1)

The SPR-based test for human cytochrome P450 51A1 (CYP51A1) ligand screening has been developed. Applicability of this system has been validated with known azole inhibitors of cytochromes P450. The studied azoles selectively interacted with human cytochrome P450 51A1, which showed the highest affini...

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Bibliographic Details
Published in:Biochemistry (Moscow). Supplement. Series B, Biomedical chemistry Biomedical chemistry, 2013-07, Vol.7 (3), p.187-195
Main Authors: 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.
Format: Article
Language:English
Subjects:
Atherosclerosis
Biochemistry
Bioorganic Chemistry
Biosensors
Chemistry
Chemistry and Materials Science
Ligands
Medicinal Chemistry
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Summary:The SPR-based test for human cytochrome P450 51A1 (CYP51A1) ligand screening has been developed. Applicability of this system has been validated with known azole inhibitors of cytochromes P450. The studied azoles selectively interacted with human cytochrome P450 51A1, which showed the highest affinity towards ketoconazole. The efficiency of the SPR based assay has been tested using 19 steroid and triterpene compounds, which have not been investigated as potential ligands of CYP51A1.
ISSN:1990-7508
1990-7516
DOI:10.1134/S1990750813030049