Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, Republic of Korea.
Appl Microbiol Biotechnol. 2013 Jul;97(13):5691-704. doi: 10.1007/s00253-013-4978-7. Epub 2013 May 30.
Bioactive natural products, such as polyketides, flavonoids, glycopeptides, and aminoglycosides, have been used as therapeutic agents. Many of them contain structurally diverse sugar moieties attached to the aglycone core structures. Glycosyltransferases (GTs) catalyze the attachment of nucleotide-activated sugar substrates to acceptor aglycones. Because these sugar moieties are usually essential for biological activity, in vivo pathway engineering in prokaryotic hosts and in vitro enzymatic approaches coupled with GT engineering are currently being used to synthesize novel glycosylated derivatives, and some of them exhibited improved biological activities compared to the parent molecules. Therefore, harnessing the potential of diverse glycosylation reactions in prokaryotes will increase the structural diversity of natural products and the possibility to generate new bioactive products.
生物活性天然产物，如聚酮、类黄酮、糖肽和氨基糖苷类，已被用作治疗剂。它们中的许多都含有结构多样的糖基部分连接在糖苷配基核心结构上。糖基转移酶（GTs）催化核苷酸活化的糖底物与受体糖苷配基的连接。由于这些糖基部分通常对生物活性至关重要，因此目前正在使用原核宿主中的体内途径工程和体外酶法结合 GT 工程来合成新型糖基化衍生物，其中一些与母体分子相比表现出改善的生物活性。因此，利用原核生物中多样化的糖基化反应的潜力将增加天然产物的结构多样性，并有可能产生新的生物活性产物。
