目的 介绍了近年来雷帕霉素及其衍生物的开发现状、作用机制与生物合成途径,探讨了通过前体定向生物合成与诱变生物合成的方式,获得雷帕霉素衍生物的研究进展,展望了雷帕霉素及衍生物的研究前景.方法 分析、归纳、总结近年来发表的相关文献.结果与结论 雷帕霉素及其衍生物是新型强效的免疫抑制剂与抗肿瘤药物,具有抗真菌、抗增殖及潜在延长哺乳动物寿命周期等作用.采用前体定向生物合成、诱变生物合成与组合生物合成的方式,可快速获得其具药理活性的衍生物.基于生物合成途径,采用系统生物学相关手段可获高产工程化菌种应用于工业化生产.%Objective The recent development situation, mechanism and biosynthesis of rapamycin and its derivatives were reviewed, and the research prospect of rapamycin and its analogs were further forecasted. Methods The literatures published in recent years were analyzed and summarized. Results and Conclusion Rapamycin and some its analogs are new potent immunosuppressive and anticancer drugs, which have obvious effects on anti-fungal, anti-proliferation, and the potential to extend the lifespan of mammalian and so on. By the ways of precursor-directed biosynthesis,mutational biosynthesis and combinatorial biosynthesis, some novel analogs of rapamycin can be obtained,and the high-yield strains tend to be reconstructed for industrial production by the means of system biology.
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