期刊
ACS CHEMICAL BIOLOGY
卷 14, 期 6, 页码 1135-1140出版社
AMER CHEMICAL SOC
DOI: 10.1021/acschembio.9b00330
关键词
-
资金
- Japan Agency for Medical Research and Development (AMED), Japan
- Ministry of Economy, Trade and Industry (METI), Japan
New technology for the derivatization of peptide natural products is required for drug development. Despite the recent advances in the genome sequencing technique enabling us to search for the biosynthetic genes for wide variety of natural products, the technical methods to get access to them are limited. A class of RiPPs, a recently emerged natural product family such as thioviridamide, is one of those possessing such unexplored chemical space. In this paper, we report a streamlined method to generate new thioviridamide derivatives and to assess their biological activities. Heterologous expression of 42 constructs in an engineered Streptomyces avermitilis host gave 35 designed thioviridamide derivatives, along with several unprecedented analogues. Moreover, cytotoxicity assay revealed that several derivatives showed more potent activities than those of prethioviridamide. These results indicate that this strategy can become one of the potential ways to produce supreme unnatural products.
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