Functional characterization of 32 CYP2C9 allelic variants

作者: Y Niinuma , T Saito , M Takahashi , C Tsukada , Mi Ito

DOI: 10.1038/TPJ.2013.22

关键词:

摘要: Genetic variations in cytochrome P450 2C9 (CYP2C9) contribute to interindividual variability the metabolism of clinically used drugs such as warfarin and tolbutamide. We functionally characterized 32 types allelic variant CYP2C9 proteins. Recombinant proteins generated using a heterologous expression system are useful for comparing functional changes expressed from low-frequency alleles. Wild-type its 31 variants were found be transiently COS-7 cells, enzymatic activity was S-warfarin representative substrate. Among tested, CYP2C9.18, CYP2C9.21, CYP2C9.24, CYP2C9.26, CYP2C9.33 CYP2C9.35 exhibited no enzyme activity, 12 showed significantly decreased activity. In vitro analysis should predicting phenotypes application personalized drug therapy.

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