The University of Auckland, 23 Symonds Street, Auckland, New Zealand.
Org Biomol Chem. 2011 Mar 7;9(5):1621-6. doi: 10.1039/c0ob01043j. Epub 2011 Jan 20.
The first synthesis of click neoglycopeptide analogues of the biologically relevant MUC1 sequence is reported. In the process, microwave-enhanced chaotrope-assisted click reaction conditions that may be used on a routine basis for the synthesis of click peptide conjugates have been developed. The convergent route for the synthesis of neoglycopeptides using these reaction conditions enables the facile, rapid, and highly efficient preparation of focused neoglycopeptide libraries of defined chemical structure for biological evaluation.
本文报道了生物相关 MUC1 序列的点击糖肽类似物的首次全合成。在此过程中,开发了微波增强变构辅助点击反应条件,这些条件可能可常规用于点击肽缀合物的合成。使用这些反应条件的糖肽的汇聚合成路线,能够实现具有明确化学结构的聚焦糖肽文库的简便、快速和高效制备,用于生物学评价。