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硅烷化标签辅助肽合成:在环境友好条件下连续一锅法延伸合成难合成的肽

Silylated Tag-Assisted Peptide Synthesis: Continuous One-Pot Elongation for the Production of Difficult Peptides under Environmentally Friendly Conditions.

作者信息

Yano Shinya, Mori Toshihiro, Kubota Hideki

机构信息

Iwate Drug Synthesis R&D Center, Sekisui Medical Co., Ltd., Iwate 028-7305, Japan.

出版信息

Molecules. 2021 Jun 8;26(12):3497. doi: 10.3390/molecules26123497.

DOI:10.3390/molecules26123497
PMID:34201337
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8228865/
Abstract

Addition of the silylated tag (STag) enables peptides to be highly soluble in CPME, allowing them to be used at high concentrations in a coupling reaction to enhance reactivity and achieve effective synthesis of sterically hindered peptides. We described the development of a continuous one-pot STag-assisted peptide synthesis platform as a method that provides near-stoichiometric, speedy, environmentally friendly, and scalable peptide synthesis.

摘要

添加硅烷化标签(STag)可使肽在环戊基甲基醚(CPME)中具有高度溶解性,从而能够在偶联反应中以高浓度使用,以增强反应活性并实现空间位阻肽的有效合成。我们描述了一种连续一锅法STag辅助肽合成平台的开发,该方法可提供接近化学计量比、快速、环保且可扩展的肽合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/9377364d7c39/molecules-26-03497-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/fe4a22721ce4/molecules-26-03497-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/5ed4adf936c0/molecules-26-03497-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/9377364d7c39/molecules-26-03497-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/fe4a22721ce4/molecules-26-03497-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/5ed4adf936c0/molecules-26-03497-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffc5/8228865/9377364d7c39/molecules-26-03497-g003.jpg

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本文引用的文献

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Macrocyclic Peptides as Drug Candidates: Recent Progress and Remaining Challenges.作为药物候选物的大环肽:最新进展和尚存的挑战。
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Orally Absorbed Cyclic Peptides.口服环肽
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Novel diphenylmethyl-derived amide protecting group for efficient liquid-phase peptide synthesis: AJIPHASE.新型二苯甲基衍生酰胺保护基用于高效液相肽合成:AJIPHASE。
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