A dual functional probe for assessing human CYP450 3A5 and 3A enzymes bioactivities

用于评估人类 CYP450 3A5 和 3A 酶生物活性的双功能探针

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作者:Fei Yan, Yonglei Cui, Yue An, Jing Ning, Xinyu Zhao, Lei Feng, Xiaokui Huo, Chao Wang, Chuanzhu Lv, Xiaochi Ma, Xiangge Tian

Aim

CYP3A5 plays a vital role in the drug metabolism, it displays varied expression levels among individuals and is easily influenced by genetic polymorphisms and some diseases. Methodology &

Conclusion

IKBA could serve as a useful tool for exploring the physiology and pathology functions of CYP3A5 and give some useful guidance for the rational use of clinical drugs.

Results

A dual function probe isobutyryl-11-keto-β-boswellic acid (IKBA) was developed; it possessed a high selectivity toward CYP3A5 and CYP3A enzymes for its two individual metabolites, respectively. The probe has the high accuracy and wide applicability in measuring the real activity of CYP3A5. Finally, IKBA was successfully used for the evaluation of the activity of CYP3A5 and CYP3A enzymes in various bio samples.

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