连接器
肽
镧硫氨酸
化学
蛋白酶
代谢物
酶
氨基酸
立体化学
环肽
生物化学
组合化学
计算机科学
操作系统
作者
Richard Morewood,Christoph Nitsche
摘要
Stapling of peptides renders them better drug candidates. We report a new peptide staple resembling the natural metabolite lanthionine ketenamine. The strategy is orthogonal to canonical amino acids, proceeds in water and allows for tailored linkers. We applied the approach to the identification of cyclic peptide inhibitiors of the Zika virus protease. The right linker length of the peptide staple proved crucial for maximising activity. The best stapled peptide showed one order of magnitude stronger enzyme inhibition than its linear analogue.
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