CYP2B6

Cytochrome P450 2B6 (CYP2B6) is a heme-thiolate monooxygenase that is part of the cytochrome P450 family, which plays a crucial role in the metabolism of drugs and xenobiotics in the body. CYP2B6 is primarily expressed in the liver and is involved in the biotransformation of a wide range of substrates, including drugs such as bupropion, efavirenz, and cyclophosphamide. Variants in CYP2B6 can also impact an individual's susceptibility to drug-induced toxicity or side effects. Inducing CYP2B6 activity can affect the metabolism and clearance of drugs that are substrates for this enzyme. Early screening for a drug candidate's potency to induce or inhibit CYP2B6 is essential for preventing potential drug failure due to toxicity or low efficacy in later stages of drug development.

Table 1 Some CYP2B6 substrates, inducers and inhibitors.

CYP2B6 Induction Assay Service

At Creative Biolabs, we offer customized CYP induction assay conditions to suit the specific requirements of each client, ensuring accurate and reliable results. Our scientists are pleased to offer a comprehensive CYP2B6 induction assay service. The service is designed to evaluate the ability of compounds to induce CYP2B6 expression. Our CYP2B6 induction assay involves culturing human hepatocytes with test compounds (inducers) for a certain period. The cells are then harvested, and the expression and activity of CYP2B6 are assessed using various techniques such as qRT-PCR and enzyme activity assays.

In a CYP2B6 induction assay, positive and negative controls are important to validate the assay and ensure the results are accurate. Positive controls in a CYP2B6 induction assay are typically compounds known to induce the expression of CYP2B6 enzymes. Whereas negative controls are compounds that are not expected to induce CYP2B6 expression. By including both positive and negative controls in our CYP2B6 induction assays, we will ensure the assay is working correctly and that any observed changes in CYP2B6 activity are due to specific induction effects.

Key features of our CYP2B6 induction assay service include:

• Precise evaluation of compound-induced CYP2B6 enzyme activity
• Comprehensive analysis of induction potential under varying conditions
• Expert guidance and data interpretation provided by our team of scientists
• Customized assay design to meet specific research needs

Support Data

Data 1: The test aims to whether Zebularine affects the CYP2B6 gene. The result indicated that Zebularine induced the expression of CYP2B6.

Host cell: HepG2 cells

Detection method: qRT-PCR

Fig.1 CYP2B6 gene expression.^1,3

Data 2: The ability of calcitriol to induce the CYP2B6 was determined by the CYP2B6 enzyme activity test. The calcitriol significantly increased CYP2B6 activity.

Host cell: Human hepatocytes or HepaRG cells

Substrate: Bupropion

Detection of metabolite: Hydroxybupropion

Analysis method: LC-MS/MS

Fig.2 CYP2B6 activity measurement.^2,3

References

1. Nakamura, Kazuaki, et al. "Zebularine upregulates expression of CYP genes through inhibition of DNMT1 and PKR in HepG2 cells."Scientific Reports 7.1 (2017): 41093.
2. Chae, Yoon-Jee, et al. "Pharmacokinetic estimation models-based approach to predict clinical implications for CYP induction by calcitriol in human cryopreserved hepatocytes and HepaRG cells." Pharmaceutics 13.2 (2021): 181.
3. Distributed under Open Access license CC BY 4.0, without modification.

For Research Use Only | Not For Clinical Use