This European patent application, published in 2013, describes the methods of biosynthetic engineering directed to produce novel medicinally important compounds of polyketide origin based on the chemobiosynthetic/mutasynthetic approach, where analogues of unnatural extender units are added into cultivation media of actinomycete cultures. These unnatural units are incorporated by the acyltransferase domain of the module 4 of FK506 polyketide synthase (fkAT4) into polyketide backbones of compounds, such as FK506 of antibiotic erythromycin, thereby incorporating novel functional groups, which cannot be introduced by usual procedures of chemical semi-synthesis. In addition, these functional groups are chemically amenable and allow for subsequent derivatization of the obtained bioactive compounds. This patent application describes in more detail the chemically reactive functional groups which are likely recognized by the fkAT4 domain and semi-synthetic possibilities that are enabled based on these functional groups.
F.02 Acquisition of new scientific knowledge
COBISS.SI-ID: 4162936