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Target intelligence / Profile preview
Cytochrome P450 2B1 (CYP2B1)
- Target
- CYP2B1
- Molecular classification
- Enzyme, Oxidoreductase, Heme enzyme
01
Overview
Cytochrome P450 2B1 (CYP2B1) is a heme-thiolate enzyme encoded by the Cyp2b1 gene in rats. It catalyzes the oxidation of structurally diverse compounds including steroids, fatty acids, and a wide array of xenobiotics and drugs, through a classic monooxygenase reaction where an oxygen atom is incorporated into the substrate. The CYP2B1 enzyme is highly flexible structurally, allowing it to accommodate and metabolize various ligands—its substrate specificity and enzymatic activity play key roles in detoxification, drug metabolism, and biotransformation. CYP2B1 is heavily studied in toxicology and pharmacology, especially for its role in bioactivation of carcinogens and drugs and as a model for the closely related human CYP2B6 isoform
- Other names
- Cyp2b-1CYPIIB1Cytochrome P450-BCytochrome P450-LM2Cytochrome P450-PB1Cytochrome P450-PB2Cytochrome P450b
02
Mechanism of action
Monooxygenation/oxidation of substrates using heme-iron center\nDrug metabolism via insertion of oxygen atom (monooxygenase reaction)\nActivation/inactivation of prodrugs, environmental chemicals, and therapeutics
03
Biological functions
Drug metabolic processSteroid hydroxylase activityFatty acid oxidationEpoxygenase P450 pathwayAromatase activity
04
Disease associations
Cancer (due to metabolization of carcinogens and chemotherapeutics)Toxicity (activation of pro-toxins, metabolism of drugs to toxic metabolites)Other (involvement in metabolism of endogenous compounds)
05
Safety considerations
Drug-drug interactions and altered pharmacokinetics due to induction/inhibitionToxic or carcinogenic metabolites produced from otherwise safe compoundsSpecies differences (rat CYP2B1 vs. human CYP2B6)
06
Interacting drugs
Bifonazole (antifungal)
3 more in the full profile.
07
Biomarkers
Induced expression (phenobarbital, other xenobiotics)Metabolite profiling for certain drug substrates
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