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    • 1. 发明申请
    • GLYCOSYLATION OF ANTIBIOTICS
    • 抗生素的糖基化
    • WO2006003456A2
    • 2006-01-12
    • PCT/GB2005002661
    • 2005-07-07
    • ISIS INNOVATIONDAVID BENJAMIN GUYGILBERT HARRY JOHN
    • DAVID BENJAMIN GUYGILBERT HARRY JOHN
    • C12P19/18C12P19/62
    • C12P19/62
    • 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.
    • 已经证明大环内酯糖基转移酶可以以高水平重组表达。 还已经证明,这些酶能够接受糖苷配基结合位点中的一系列平面,环状疏水性分子,使得它们可以用于使一系列底物糖基化。 已经进一步证明这些酶在供体糖识别中显示出可塑性,使得它们可以用于将新的糖装饰物引入生物活性分子中。 因此,本发明提供了将糖附着于底物的方法,包括在糖供体存在下使糖与大环内酯糖基转移酶接触。 本发明还提供了以高水平重组表达大环内酯糖基转移酶的方法,包括在细菌宿主细胞中表达编码酶的多核苷酸。