Department of Chemistry, Indian Institute of Science Education and Research , Dr. Homi Bhabha Road, Pune 411008, India.
Org Lett. 2015 Jan 16;17(2):230-3. doi: 10.1021/ol503310r. Epub 2014 Dec 24.
The synthesis and utilization of novel thiostatines (β-SH-substituted γ-amino acids) in the design of backbone-disulfide-stabilized β-hairpin mimetics, solution conformations of hybrid β-hairpins and Cys-disulfide-stabilized α-peptide analogue, their thiol exchange, and proteolytic stability are investigated. The results suggest that thiostatines can be used to design proteolytically stable water-soluble β-hairpin mimetics without deviating from overall β-hairpin conformation.
新型硫缩氨酸（β-SH 取代的 γ-氨基酸）的合成与利用在设计骨干二硫键稳定的β-发夹模拟物、杂合β-发夹和 Cys-二硫键稳定的α-肽类似物的溶液构象、它们的巯基交换和蛋白水解稳定性方面进行了研究。结果表明，硫缩氨酸可用于设计蛋白水解稳定的水溶性β-发夹模拟物，而不会偏离整体β-发夹构象。
