Abstract
A new method for the pre-activation cyclization of a long peptide is described. The approach involves the formation of a pre-activated succinimidyl ester species in advance of amidation, which completely eliminates the potentially troublesome amine end-capping side reaction. The cyclization reactions proceed with high efficiency and fast reaction kinetics for the long peptide with 25 residues. The exploration and large-scale preparation of synthetic cyclic peptides should become more accessible and feasible with this approach. This method has a potential to be further applied for the synthesis of much longer and more complex cyclic peptides.
| Original language | English |
|---|---|
| Pages (from-to) | 5335-5338 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 25 |
| Issue number | 22 |
| DOIs | |
| Publication status | Published - 2015 Nov 15 |
All Science Journal Classification (ASJC) codes
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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Choi, S. H., Jeong, W. J., Choi, S. J., & Lim, Y. B. (2015). Highly efficient and fast pre-activation cyclization of the long peptide: Succinimidyl ester-amine reaction revisited. Bioorganic and Medicinal Chemistry Letters, 25(22), 5335-5338. https://doi.org/10.1016/j.bmcl.2015.09.038