Recombinant enzymes represent a useful test system for studies requiring high levels of catabolic activity and the simplest system available to study interactions between a drug candidate and individual enzymes. These recombinant enzymes can be used in many in vitro assays, and are particularly useful in reaction phenotyping and enzyme inhibition preclinical studies.
Recombinant Enzymes for Drug Discovery & Preclinical Development
Human & Animal Recombinant Enzymes
We offer multiple recombinant enzyme bactosome (enzymes expressed in E. coli bacteria) products to support drug discovery and preclinical drug development services: Classic Bactosomes and EasyCYPs. Classic Bactosomes (1 nmol volume) allow customers to pair specific enzyme activities with various levels of reductase and activity rate linearity. EasyCYPs are standardized human CYP bactosomes provided in a standard concentration (1 nmol/mL), standard protein concentration (10 mg/mL) and a standard vial size (0.5 nmol).
Human Recombinant CYPs: Classic Bactosomes vs EasyCYPs
E. coli expressed recombinant enzymes, or Bactosomes, exhibit greater activity levels and turnover numbers when compared to CYPs expressed from insect cells, or Supersomes. Bactosomes show excellent linearity over time, allowing longer incubations and generating better results and can be optimized for various study types. Our selection includes Classic Bactosomes for a wide variety of CYP enzymes with differing levels of reductase and b5. Classic Bactosomes show excellent linearity over time, allowing longer incubations and generating better results.
Similar to Classic Bactosomes, EasyCYPs are offered for a wide variety of human CYP enzymes in low or high reductase and with or without b5. EasyCYPs boast standard CYP concentration, standard protein concentration, and standard vial size, and are commonly used for in vitro inhibition, metabolism, reaction phenotyping, and metabolite generation studies.
Cypex Classic Bactosome & EasyCYP Features
- Patented E. coli expression system
- Excellent batch-to-batch consistency
- Patented production method for native, or minimally modified P450s
- Robust P450 activity levels, representative of human enzymes
- Extensive batch-specific data
- Available in high, medium or low reductase and with or without b5
- Standardized for ultimate convenience (EasyCYPs)
- Market-leading linearity
Recombinant CYPs, UGTs, SULTs, and other enzymes for use in drug discovery and preclinical development assays
Different isoforms of recombinant CYPs and UGTs are engineered to enable researchers to distinguish a xenobiotic’s effect on the activity of individual enzymes. Some enzymes, such as CYP3A4 and CYP3A5, are very similar in structure and are hard to distinguish in LC/MS analysis. Recombinant enzymes, therefore, are most often used to confirm any ambiguity observed in reaction phenotyping studies using complex mixtures of enzymatic activities. In cases of low metabolism, recombinant enzymes can be used at high concentrations to amplify metabolic activity for use in metabolic stability screening and inhibitory potential evaluation. Both recombinant CYPs and UGTs can be helpful for these applications, and through Cypex we are pleased to offer our customers an exceptionally wide selection of recombinant human and animal enzymes.