Abstract
Cyclization confers several advantages to peptides, cumulatively serving to make them more drug-like. In this protocol, cyclic peptides are generated via bis-alkylation of cysteine-containing peptides using α,α′-dibromo-m-xylene. The reactions are robust and high yielding. Multiple reaction platforms for the application of this versatile strategy are described herein: the cyclization of solid-phase-synthesized peptides, both in solution and on resin, as well as the cyclization of in vitro translated mRNA-peptide fusion libraries on oligo(dT) resin.
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Acknowledgments
This work was supported by grants from the Concern Foundation and the NIH (1R01CA166264).
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Hacker, D.E., Almohaini, M., Anbazhagan, A., Ma, Z., Hartman, M.C.T. (2015). Peptide and Peptide Library Cyclization via Bromomethylbenzene Derivatives. In: Derda, R. (eds) Peptide Libraries. Methods in Molecular Biology, vol 1248. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2020-4_8
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DOI: https://doi.org/10.1007/978-1-4939-2020-4_8
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