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Synthesis of Asparagusic Acid Modified Lysine and its Application in Solid-Phase Synthesis of Peptides with Enhanced Cellular Uptake
Synlett ( IF 1.7 ) Pub Date : 2017-12-08 , DOI: 10.1055/s-0036-1591847
Pablo Rivera-Fuentes , Alina Tirla , Moritz Hansen

Cyclic disulfides, such as asparagusic acid, enhance the uptake of a variety of cargoes into live cells. Here, we report a robust and scalable synthesis of an asparagusic acid modified lysine. This amino acid can be used in solid-phase peptide synthesis. We confirmed that incorporation of this building block into the sequence of a peptide increases its cellular uptake substantially.

中文翻译:

天门冬氨酸修饰赖氨酸的合成及其在固相合成增强细胞摄取肽中的应用

环状二硫化物,如天门冬氨酸,可增强多种物质对活细胞的吸收。在这里,我们报告了天冬氨酸修饰赖氨酸的稳健且可扩展的合成。该氨基酸可用于固相肽合成。我们证实,将此构建块并入肽序列中可显着增加其细胞摄取。
更新日期:2017-12-08
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