| Autor: |
Chen H; Department of Chemistry, State University of New York, University at Albany, Albany, New York 12222, United States., Zhang Q; Department of Chemistry, State University of New York, University at Albany, Albany, New York 12222, United States. |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of the American Chemical Society [J Am Chem Soc] 2023 Dec 20; Vol. 145 (50), pp. 27218-27224. Date of Electronic Publication: 2023 Dec 11. |
| DOI: |
10.1021/jacs.3c10341 |
| Abstrakt: |
Chemical synthesis offers robust tactics for structural alterations of peptides and proteins. It remains a labor-intensive and complex process due to the challenges in selectively modifying diverse amino acid side chains and termini. Direct α-peptide ligation without premodification is a significant hurdle, especially when aiming to include all proteinogenic amino acids at the ligation site. We introduce Native Peptide Cyclization (NPC), a chemoselective method enabling intramolecular peptidyl ligation without the need for premodification. NPC cyclizes unprotected linear peptides through controlled, sequential C- and N-terminal activation via pH modulation. Water-based NPC simplifies peptide ligation, easing the labor-intensive nature of peptide synthesis, aiding efficient cyclic peptide preparation and enabling cost-effective macrocycle-based therapeutics. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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