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

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

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

Biomed Khim ; 59(4): 388-98, 2013.

Article em Ru | MEDLINE | ID: mdl-24502137

ABSTRACT

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.

Assuntos

Inibidores de 14-alfa Desmetilase/química; Técnicas Biossensoriais; Cetoconazol/química; Esterol 14-Desmetilase/química; Inibidores de 14-alfa Desmetilase/metabolismo; Humanos; Cetoconazol/metabolismo; Ligação Proteica; Esterol 14-Desmetilase/metabolismo

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Base de dados: MEDLINE Assunto principal: Técnicas Biossensoriais / Esterol 14-Desmetilase / Inibidores de 14-alfa Desmetilase / Cetoconazol Idioma: Ru Ano de publicação: 2013 Tipo de documento: Article

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