期刊
CHEMBIOCHEM
卷 16, 期 18, 页码 2646-2650出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201500494
关键词
click chemistry; cyclic peptides; enzymatic reactions; macrocyclisation; patellamides
资金
- European Research Council [339367]
- UK Biotechnology and Biological Sciences Research Council [K015508/1]
- Wellcome Trust [094476, 079272AIA, 097831]
- Royal Society
- Biotechnology and Biological Sciences Research Council [BB/K015508/1] Funding Source: researchfish
- Engineering and Physical Sciences Research Council [1245361, 1647607] Funding Source: researchfish
- BBSRC [BB/K015508/1] Funding Source: UKRI
Many natural cyclic peptides have potent and potentially useful biological activities. Their use as therapeutic starting points is often limited by the quantities available, the lack of known biological targets and the practical limits on diversification to fine-tune their properties. We report the use of enzymes from the cyanobactin family to heterocyclise and macrocyclise chemically synthesised substrates so as to allow larger-scale syntheses and better control over derivatisation. We have made cyclic peptides containing orthogonal reactive groups, azide or dehydroalanine, that allow chemical diversification, including the use of fluorescent labels that can help in target identification. We show that the enzymes are compatible and efficient with such unnatural substrates. The combination of chemical synthesis and enzymatic transformation could help renew interest in investigating natural cyclic peptides with biological activity, as well as their unnatural analogues, as therapeutics.
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