PolyCYPs Kits for Late-Stage Oxidation
There are two screening kit options – a 20 enzyme kit containing 18 PolyCYPs isoforms, aldehyde oxidase (AOX) and flavo-containing monooxygenase 3 (FMO3) and an 8-enzyme “Diversification kit” containing 8 promiscuous PolyCYP enzymes.
Content of PolyCYPs oxidation screening kit
All reagents are provided as lyophilised powders in sealed vials together with a 24-well reaction plate and air-permeable seal.
Everything is included in the kit that you will need to perform the reaction in your lab, just add your compounds and water!
PolyCYP enzyme reactions are fully scalable from mg to gram quantities through a number of routes, either by resupply of lyophilised enzymes for mg scale production in house, or larger scale production at gram scale at Hypha, with optional purification and structure elucidation.
Multiple 10ml scale-up vials, suitable for converting 1mg of parent compound per vial, can be ordered off-the-shelf for any isoform for in-house scale-up in a kit format. Co-factors and formulant are also included, along with a 24-well block suitable for performing 4 x 2.5 ml reactions. Other incubation formats can also be used, as recommended in the kit instructions.
For larger quantities of any PolyCYPs products, we offer reactions undertaken at Hypha using cell paste from the recombinant E.coli or streptomycete clones containing the enzyme of interest.
Hypha can also undertake screening of drug compounds using PolyCYPs enzymes on behalf of a client in a service called PolarExplorer. We offer a flexible end-to-end service including scale-up, purification and structure elucidation. Alternatively, scale-up reactions can be conducted at Hypha and products provided to the client for purification and/or structure elucidation.
Why use PolyCYPs oxidation kits?
Introducing oxygen into a drug candidate late in the optimisation process has several applications including exploration of SAR (structure-activity relationships) and the ability to access derivatives that may possess superior properties such as improved metabolic stability and LLE (ligand-lipophilicity efficiency). Biocatalysis can provide access to chemical space in a complementary manner to chemical synthesis and provide a “one-experiment” solution to accessing multiple derivatives in parallel. This poster illustrates the application of a new biocatalysis kit, PolyCYPs®, to enable parallel synthesis of hydroxylated derivatives of drugs.
This poster illustrates the application of a new biocatalysis kit, PolyCYPs®, to enable scalable synthesis of CYP-derived metabolites of drugs. The PolyCYPs platform is comprised of a set of recombinant cytochrome P450 enzymes and redox partners cloned from some of the talented actinomycetes in Hypha’s biotransformation panel. Enzymes in the kit catalyze the oxidation of a wide variety of substrate types to generate multiple mammalian and microbial-derived CYP metabolites.
A cell-free kit of cytochrome P450 enzymes and ferredoxin/ferredoxin reductase redox partners, termed PolyCYPs®, is being developed for generating scalable quantities of oxidised metabolites. P450 cytochromes in the kit have been derived from some of Hypha’s most talented biotransforming bacteria and are capable of generating human and other mammalian metabolites of drug compounds.
“We would like to mention that it has been a pleasure to work with Hypha in this project. We are really satisfied with how the collaboration has progressed, reaching the defined goals and timelines in a very efficient manner. Access of hydroxylated compounds through PolyCYPs has saved our company time and resources. We are sure that we will have more opportunities to work together in the future.”
European Pharma Company
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Hypha Discovery is a UK-based CRO supporting pharmaceutical and agrochemical companies worldwide through the production of metabolites and new derivatives of drugs and agrochemicals in discovery and development.