State Key Laboratory of Bioorganic and Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.
Org Biomol Chem. 2018 Dec 12;16(48):9373-9376. doi: 10.1039/c8ob02665c.
Using a highly effective heterologous expression system, the YM-216391 (1) biosynthetic gene cluster was engineered to yield aurantizolicin (2) and the hybrid compound 3. Both of these compounds were isolated and fully structurally characterised and the bioactivity was evaluated. The results indicate that compound 3 exhibits significantly improved antitumor activity.
采用高效的异源表达系统，对 YM-216391（1）生物合成基因簇进行了工程改造，以生成 aurantizolicin（2）和杂合化合物 3。这两种化合物均已分离并进行了充分的结构表征，并对其生物活性进行了评估。结果表明，化合物 3 表现出显著改善的抗肿瘤活性。
