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Ligation Technologies for the Synthesis of Cyclic Peptides

机译:结扎技术的合成循环肽

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摘要

Cyclic peptides have been attracting a lot of attention in recent decades, especially in the area of drug discovery, as more and more naturally occurring cyclic peptides with diverse biological activities have been discovered. Chemical synthesis of cyclic peptides is essential when studying their structure-activity relationships. Conventional peptide cyclization methods via direct coupling have inherent limitations, like the susceptibility to epimerization at the C-terminus, poor solubility of fully protected peptide precursors, and low yield caused by oligomerization. In this regard, chemoselective ligation-mediated cyclization methods have emerged as effective strategies for cyclic peptide synthesis. The toolbox for cyclic peptide synthesis has been expanded substantially in the past two decades, allowing more efficient synthesis of cyclic peptides with various scaffolds and modifications. This Review will explore different chemoselective ligation technologies used for cyclic peptide synthesis that generate both native and unnatural peptide linkages. The practical issues and limitations of different methods will be discussed. The advance in cyclic peptide synthesis will benefit the biological and medicinal study of cyclic peptides, an important class of macrocycles with potentials in numerous fields, notably in therapeutics.
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  • 来源
    《Chemical Reviews》 |2019年第17期|共31页
  • 作者单位

    Univ Hong Kong State Key Lab Synthet Chem Dept Chem Pokfulam Rd Hong Kong Peoples R China;

    Univ Hong Kong State Key Lab Synthet Chem Dept Chem Pokfulam Rd Hong Kong Peoples R China;

    Univ Edinburgh Sch Chem Edinburgh EH8 9LE Midlothian Scotland;

    Univ Hong Kong State Key Lab Synthet Chem Dept Chem Pokfulam Rd Hong Kong Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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