Late stage hydroxylation using PolyCYPs® enzymes
Hypha’s PolyCYPs® enzymes provide a fast and easy way to hydroxylate aliphatic or aromatic moieties at multiple sites in parallel, including metabolically susceptible positions. Both CYP-derived human metabolites and other oxidised derivatives can then be accessed simultaneously for structure elucidation and biological testing.
PolyCYPs® enzymes in the kit have been cloned 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.
In this case study, five active monohydroxylated derivatives of a client’s drug lead were produced using PolyCYPs, with a 56% conversion of the parent drug by the best PolyCYP enzyme, enabling access to polar chemical space in parallel as part of SAR studies. Access a pdf of the poster on “Late Stage Functionalization of Drug Candidates using PolyCYPS® Enzymes” here.
Drug candidates are screened in client labs against PolyCYPs enzymes in the screening kit to identify isoforms undertaking the desired oxidation(s). For lipophilic compounds, a cyclodextrin-based formulation reagent is included to aid solubilisation. Scale-up vials of any specific isoform can then be ordered to generate more material for further testing. This process can also be operated at Hypha as a service option if preferred.
For more information or to order a kit, email firstname.lastname@example.org