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REVERSIBLE NATURAL PRODUCT GLYCOSYLTRANSFERASE-CATALYZED REACTIONS, COMPOUNDS AND RELATED METHODS

机译:可逆天然产物糖基转移酶催化的反应,化合物及相关方法

摘要

The present invention relates to methods of use of glycosyltransferases and related novel compounds. The invention exploits the reversibility of glycosyltransferases to generate new sugars, unnatural biomolecules and numerous one-pot reactions for generation of new biomolecules having varied backbones such as enediynes, vancomycins, bleomycins, anthracyclines, macrolides, pluramycins, aureolic acids, indolocarbazoles, aminglycosides, glycopeptides, polyenes, coumarins, benzoisochromanequinones, calicheamicins, erythromycin, avermectins, ivermectins, angucyclines, cardiac glycosides, steroids or flavinoids. In preferred embodiments, the invention specifically relates to biosynthesis of anticancer (the enediyne calicheamicin, CLM), anthelmintic agents (the macrolides avermectin, ivermectin and erythromycin) and antibiotic (the glycopeptide vancomycin, VCM) natural product-based drugs developed by reversible, bidirectional glycosyltransferase-catalyzed reactions.
机译:本发明涉及糖基转移酶和相关新化合物的使用方法。本发明利用糖基转移酶的可逆性来产生新的糖,非天然生物分子和大量的一锅法反应,以产生具有各种主链的新生物分子,所述主链例如烯二炔,万古霉素,博来霉素,蒽环类,大环内酯类,普拉霉素,金黄色酸,吲哚并咔唑类,吲哚并咔唑类,a ,多烯,香豆素,苯并异铬烷醌,加利车霉素,红霉素,阿维菌素,伊维菌素,安古环素,强心苷,类固醇或类黄酮。在优选的实施方案中,本发明具体涉及通过可逆的双向开发的基于天然产物的抗癌药物(烯二炔加利车霉素,CLM),驱虫药(大环内酯阿维菌素,伊维菌素和红霉素)和抗生素(糖肽万古霉素,VCM)的天然合成。糖基转移酶催化的反应。

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