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- W2914149134 abstract "Disulfide-rich macrocyclic peptides—cyclotides, for example—represent a promising class of molecules with potential therapeutic use. Despite their potential their efficient synthesis at large scale still represents a major challenge. Here we report new chemoenzymatic strategies using peptide ligase variants—inter alia, omniligase-1—for the efficient and scalable one-pot cyclization and folding of the native cyclotides MCoTI-II, kalata B1 and variants thereof, as well as of the θ-defensin RTD-1. The synthesis of the kB1 variant T20K was successfully demonstrated at multi-gram scale. The existence of several ligation sites for each macrocycle makes this approach highly flexible and facilitates both the larger-scale manufacture and the engineering of bioactive, grafted cyclotide variants, therefore clearly offering a valuable and powerful extension of the existing toolbox of enzymes for peptide head-to-tail cyclization." @default.
- W2914149134 created "2019-02-21" @default.
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- W2914149134 date "2019-04-25" @default.
- W2914149134 modified "2023-09-24" @default.
- W2914149134 title "Efficient Enzymatic Cyclization of Disulfide‐Rich Peptides by Using Peptide Ligases" @default.
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- W2914149134 doi "https://doi.org/10.1002/cbic.201900033" @default.
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