Recent advancements in drug development have highlighted the importance of understanding the Cytochrome P450 (CYP) enzyme system encoded by the P450 gene family. This system plays a crucial role in drug metabolism, with certain drugs being metabolized by multiple CYP isozymes. Variability in the expression and activity of these enzymes among individuals, species, and ethnic groups can lead to differences in drug response and potential for drug-drug interactions. To address these challenges, researchers have developed a fluorescence-based High-Throughput Screening (HTS) assay using recombinant human CYP2B6 and novel fluorogenic substrates. This assay enables the rapid screening of a large panel of compounds for CYP2B6 metabolism and inhibition. By utilizing advanced screening techniques like HTS, researchers aim to improve the efficiency and safety of drug discovery processes by identifying potential metabolic issues early in development. These innovative approaches not only enhance our understanding of drug metabolism but also pave the way for the design of safer and more effective drugs for diverse patient populations.
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