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Future Med Chem. 2019 Nov;11(22):2891-2903. doi: 10.4155/fmc-2019-0173. Epub 2019 Nov 8.

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

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Academy of Integrative Medicine, College of Pharmacy, The National & Local Joint Engineering Research Center for Drug Development of Neurodegenerative Disease, Dalian Medical University, Dalian 116044, PR China.
Preparation Department, Ningxia Hui Autonomous Region Hospital of Traditional Chinese Medicine, Yinchuan 750021, PR China.
Clinical Laboratory, The Second Affiliated Hospital of Dalian Medical University, No. 467 Zhongshan Road, Shahekou District, Dalian City, Liaoning Provinc, PR China.
Institute of Functional Materials & Molecular Imaging, College of Emergency & Trauma, Hainan Medical University, No. 3 Xueyuan Road, Longhua District, Haikou, Hainan, PR China.


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 & 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. 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.


3-isobutyryl-11-keto-β-boswellic acid; CYP3A5; dual functional probe; high selectivity


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