Abstract
Macrocyclization is a valuable tool for drug design and protein engineering. Although various methods have been developed to prepare macrocycles, a general and efficient strategy is needed. Here we report a highly efficient method using butelase 1 to macrocyclize peptides and proteins ranging in sizes from 26 to >200 residues. We achieved cyclizations that are 20,000 times faster than sortase A, the most widely used ligase for protein cyclization. The reactions completed within minutes with up to 95% yields.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Animals
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Cyclization
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Humans
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Ligases / chemistry
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Ligases / metabolism*
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Models, Molecular
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Molecular Sequence Data
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Peptide Synthases / chemistry
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Peptide Synthases / genetics
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Peptide Synthases / metabolism
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Peptides / chemistry
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Peptides / metabolism*
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Plant Proteins / chemistry
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Plant Proteins / genetics
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Plant Proteins / metabolism
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Proteins / chemistry
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Proteins / metabolism*
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Rats
Substances
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Peptides
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Plant Proteins
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Proteins
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Ligases
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Peptide Synthases