Cypex Expands Portfolio of Recombinant Enzymes

As a distributor for Cypex in the US and Canada, XenoTech is proud to offer this portfolio of products based on patented technology. As a leader in the study and support of xenobiotic metabolism, XenoTech brings an unsurpassed combination of Quality, Convenience, and Selection of test systems for DMPK research. Cypex shares these values and assists in the delivery of a comprehensive offering.

Most drug metabolism occurs in the liver. Enzymes located in liver cells (hepatocytes) protect the organism against an accumulation of lipid-soluble exogenous and endogenous compounds by converting them to water-soluble metabolites which can be easily excreted by the kidney. Thus using a quality source of enzymes in research is imperative to ensuring proper development and testing of drugs and chemicals.

Cypex offers an extensive portfolio of Cytochrome P450 (CYP) enzymes (Bactosomes) prepared using their patented technique involving expression in E. coli, rather than in insect cells. The recombinant enzymes, available as preparations with activity levels similar to those found in vivo, or as preparations with a high activity, are ideal test systems for preclinical reaction phenotyping and inhibition studies.

Cypex has a large portfolio of Bactosomes for drug development with an extensive number of CYPs from human, dog, mouse, and monkey. For drug development, human CYPs have been well characterized for specific inhibitors and substrates of phenotyping and inhibition, but animal CYPs have not. Therefore Cypex has recently added a range of porcine CYPs to complement the canine CYPs that can be used for veterinary medicine development. These recombinants offer insight as to which enzymes are involved in metabolism and which might cause interaction issues. Currently there are 9 dog and 5 pig CYPs available with more being developed. Specific enzyme information is available on our website and www.cypex.co.uk.

Related information:

• Poster: Development of Fluorogenic Assays for Determining IC50 Values for NCEs with a Panel of Canine Cytochrome P450s, Incorporating IC50 Changes Over Time to Predict Time / Metabolism Dependent Inhibition
• Poster: Expression of Four Porcine CYPs in E. Coli and Development of Fluorogenic CYP Inhibition Assays
• Paper: Current Cytochrome P450 Phenotyping Methods Applied to Metabolic Drug-Drug Interaction Prediction in Dogs
• Paper: Evaluation of Escherichia coli Membrane Preparations of Canine CYP1A1, 2B11, 2C21, 2C41, 2D15, 3A12, and 3A26 with Coexpressed Canine Cytochrome P450 Reductase

In the agrochemical industry, CYPs have been implicated in conferring resistance to insecticides. To address this, Cypex has begun expressing insect CYPs. To date the range includes mosquito CYPs and CYPs from two commercial pest species (B tabaci (white fly) and T.urticae (spider mite)) for which four CYPs thought to be involved in insecticide resistance have been produced. Screening new compounds for metabolism by these enzymes would enable companies to flag compounds that have potential resistance liabilities (helping to prevent failure later on). These CYPs are available at the moment as a custom order. Further insect CYP isoforms will be produced and Cypex is happy to undertake contract development work to express enzymes that do not form part of its current portfolio.

Related information:

• Poster: Recombinant CYP6M2 Inhibition by Insecticides Recommended by WHO for Indoor Residual Spraying

Other enzymes that Cypex has produced on a contract basis include CYPs which are drug / fungicide targets. These are being used to look for positive hits for new compounds, or to eliminate new compounds that target a protein for which drug resistance is beginning to emerge. Enzymes that are available as custom preparations include CYP51A1 (rat and human), CYP26A1 (human, cynomolgus and zebrafish), CYP26B1 (human) and CYP2F2 (mouse), CYP51 (T. cruzi).

Related information:

• Poster: Development of a Fast, Fluorescence Based Screen for Inhibition of B. Tabaci, and T. Urticae Cytochrome P450s
• Paper: Development of a Fluorescence-based Trypanosoma cruzi CYP51 Inhibition Assay for Effective Compound Triaging in Drug Discovery Programmes for Chagas Disease

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