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A highly selective probe for human cytochrome P450 3A4: isoform selectivity, kinetic characterization and its applicationsElectronic supplementary information (ESI) available: Materials and methods, enzyme sources, analytical instruments and conditions, inhibition assays, correlation studies, and docking simulation. See DOI: 10.1039/c3cc45250f

Bufalin 5β-hydroxylation was found to be an isoform-specific biotransformation probe substrate for cytochrome P450 3A4 (CYP3A4). The probe reaction was well-characterized and it can be used for measuring the real catalytic activities of CYP3A4 from different enzyme sources. An isoform-specific biotr...

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Main Authors: Ge, Guang-Bo, Ning, Jing, Hu, Liang-Hai, Dai, Zi-Ru, Hou, Jie, Cao, Yun-Feng, Yu, Zhen-Wen, Ai, Chun-Zhi, Gu, Jing-Kai, Ma, Xiao-Chi, Yang, Ling
Format: Article
Language:English
Online Access:Get full text
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Summary:Bufalin 5β-hydroxylation was found to be an isoform-specific biotransformation probe substrate for cytochrome P450 3A4 (CYP3A4). The probe reaction was well-characterized and it can be used for measuring the real catalytic activities of CYP3A4 from different enzyme sources. An isoform-specific biotransformation by human cytochrome P450 3A4 (CYP3A4) has been characterized and reported for the first time.
ISSN:1359-7345
1364-548X
DOI:10.1039/c3cc45250f