Robertson Naomi S, Walsh Stephen J, Fowler Elaine, Yoshida Masao, Rowe Sam M, Wu Yuteng, Sore Hannah F, Parker Jeremy S, Spring David R
Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, CB2 1EW, UK.
Chem Commun (Camb). 2019 Aug 7;55(64):9499-9502. doi: 10.1039/c9cc05042f.
We report a novel divinyltriazine linker for the stapling of two cysteine residues to form macrocyclic peptides from their unprotected linear counterparts. The stapling reaction occurred rapidly under mild conditions on a range of unprotected peptide sequences. The resulting constrained peptides displayed greater stability in a serum stability assay when compared to their linear counterparts.
我们报道了一种新型的二乙烯基三嗪连接体，用于连接两个半胱氨酸残基，从而从其未受保护的线性对应物形成大环肽。在温和条件下，该连接反应能在一系列未受保护的肽序列上快速发生。与线性对应物相比，所得的受限肽在血清稳定性测定中表现出更高的稳定性。
