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High-Throughput 2018, 7(4), 29;

Current High-Throughput Approaches of Screening Modulatory Effects of Xenobiotics on Cytochrome P450 (CYP) Enzymes

Department of Biomedical Science, the University of Nottingham Malaysia Campus, Jalan Broga, Semenyih 43500, Selangor, Malaysia
School of Pharmacy, International Medical University, Bukit Jalil 57000, Wilayah Persekutuan Kuala Lumpur, Malaysia
Author to whom correspondence should be addressed.
Received: 24 August 2018 / Revised: 10 September 2018 / Accepted: 26 September 2018 / Published: 29 September 2018
PDF [970 KB, uploaded 29 September 2018]


Cytochrome P450 (CYP) is a critical drug-metabolizing enzyme superfamily. Modulation of CYP enzyme activities has the potential to cause drug–drug/herb interactions. Drug–drug/herb interactions can lead to serious adverse drug reactions (ADRs) or drug failures. Therefore, there is a need to examine the modulatory effects of new drug entities or herbal preparations on a wide range of CYP isoforms. The classic method of quantifying CYP enzyme activities is based on high-performance liquid chromatography (HPLC), which is time- and reagent-consuming. In the past two decades, high-throughput screening methods including fluorescence-based, luminescence-based, and mass-spectrometry-based assays have been developed and widely applied to estimate CYP enzyme activities. In general, these methods are faster and use lower volume of reagents than HPLC. However, each high-throughput method has its own limitations. Investigators may make a selection of these methods based on the available equipment in the laboratory, budget, and enzyme sources supplied. Furthermore, the current high-throughput systems should look into developing a reliable automation mechanism to accomplish ultra-high-throughput screening in the near future. View Full-Text
Keywords: high-throughput screening; inhibitory effects; cytochrome P450; in vitro high-throughput screening; inhibitory effects; cytochrome P450; in vitro

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Ung, Y.T.; Ong, C.E.; Pan, Y. Current High-Throughput Approaches of Screening Modulatory Effects of Xenobiotics on Cytochrome P450 (CYP) Enzymes. High-Throughput 2018, 7, 29.

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