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High-Throughput 2018, 7(4), 29; https://doi.org/10.3390/ht7040029

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

1
Department of Biomedical Science, the University of Nottingham Malaysia Campus, Jalan Broga, Semenyih 43500, Selangor, Malaysia
2
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
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PDF [970 KB, uploaded 29 September 2018]
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Abstract

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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