Van't Hoff Institute for Molecular Sciences, University of Amsterdam, Science Park 904, 1098 XH Amsterdam, The Netherlands.
Org Lett. 2012 Mar 2;14(5):1194-7. doi: 10.1021/ol203259a. Epub 2012 Feb 14.
The synthesis and applications of water-soluble scaffolds that conformationally constrain side chain unprotected linear peptides containing two cysteines are described. These scaffolds contain a functionality with orthogonal reactivity to be used for labeling and ligation. This is illustrated by the chemical ligation of two dissimilar constrained peptides via oxime ligation or strain-promoted azide-alkyne cycloaddition in aqueous media.
水溶性支架的合成及其应用，该支架可使含有两个半胱氨酸的侧链未保护线性肽构象受限。这些支架包含一种具有正交反应性的官能团，可用于标记和连接。通过肟连接或在水相介质中促张力促进的叠氮化物-炔烃环加成反应，将两种不同的约束肽进行化学连接，即可说明这一点。
