On Demand Attachment and Detachment of rac-2-Br-DMNPA Tailoring to Facilitate Chemical Protein Synthesis
On Demand Attachment and Detachment of rac-2-Br-DMNPA Tailoring to Facilitate Chemical Protein Synthesis
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按需附着和分离 rac-2-Br-DMNPA 定制以促进化学蛋白质合成
DOI：
10.1021/acs.orglett.1c02295
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发表时间：
2021
期刊：
影响因子：
5.2
通讯作者：
He Chunmao
中科院分区：
文献类型：
--
作者：
Zhang Yuqi;Chen Junlang;He Chunmao
本研究开发了一种双功能半胱氨酸后期保护试剂rac-2-Br-DMNPA 2。通过鉴定itst-Bu ester 1在连接条件下为更有竞争力的形式，完成了模型肽和蛋白质的容易的N-末端和侧链笼化。在此基础上，一锅连接和光解策略应用于合成的微小蛋白质的氯毒素。更重要的是，我们扩展了2作为一个双功能接头的无痕固相化学连接的效用。
Herein, we developed a bifunctional reagentrac-2-Br-DMNPA2for the late-stage protection of peptide cysteine. Through the identification of itst-Bu ester1as a more competent form under ligation conditions, facile N-terminal and side-chain caging for the model peptide and protein were accomplished. Building upon this, a one-pot ligation and photolysis strategy was applied in the synthesis of the mini-protein chlorotoxin. More importantly, we extended the utility of2as a bifunctional linker for traceless solid-phase chemical ligation.