GLYCOSYLATION OF ANTIBIOTICS

摘要

It has been demonstrated that macrolide glycosyltransferase enzymes can be recombinantly expressed at high levels. It has also been demonstrated that that these enzymes are able to accept a range of planar, cyclic, hydrophobic molecules in the aglycone binding site such that they may be used to glycosylate a range of substrates. It has been further demonstrated that these enzymes display a plasticity in donor sugar recognition such that they may be utilitised in introducing novel sugar decorations into bioactive molecules. Accordingly, the invention provides a method of attaching a sugar to a substrate comprising contacing the sugar with a macrolide glycosyltransferase enzyme in the presence of a sugar donor. The invention also provides a method of recombinantly expressing a macrolide glycosyltransferase enzyme at a high level comprising expressing a polynucleotide encoding the enzyme in a bacterial host cell.