PolyCYPs® diversification kits

PolyCYPs® diversification kits

Small changes to a structure through late stage functionalisation efforts can have a large impact in achieving improved LLE and solubility of drugs. Hydroxyl groups are the most common functional group in drugs and can reduce clogP by >1 unit, as well as enhance metabolic stability. Other benefits such as increased potency and greater selectivity are also achievable through late stage hydroxylation.

Hypha’s PolyCYPs® diversification kit is a fast and easy way to hydroxylate aliphatic or aromatic moieties at multiple sites in parallel, including metabolically susceptible positions. Both CYP-mediated human metabolites and other oxidised derivatives can then be evaluated simultaneously.

New to the market, Hypha’s PolyCYPs® enzymes have been mined from some of the talented actinomycete bacteria in Hypha’s biotransformation panel, providing a wide diversity of CYPs that hydroxylate a variety of drug compounds.

PolyCYPs® enzymes catalyse the production of both metabolites and oxidised analogues of drugs, illustrated in the box on the right (click to expand) for valsartan and ritonavir where metabolites and novel derivatives are synthesised by different PolyCYPs, providing an opportunity to access these for characterisation and biological testing.

Lead diversification case study

In one case study, five active monohydroxylated derivatives of a client’s drug lead were produced using enzymes in the diversification kit, with a 56% conversion of the parent drug by the best PolyCYP, enabling access to polar chemical space in parallel as part of SAR studies.

Download a pdf of the PolyCYPs brochure.

For more information or to order a kit, email enquiries@hyphadiscovery.co.uk

 

 

 

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