Frontispiece: Perfluoroaryl and Perfluoroheteroaryl Reagents as Emerging New Tools for Peptide Synthesis, Modification and Bioconjugation
Frontispiece: Perfluoroaryl and Perfluoroheteroaryl Reagents as Emerging New Tools for Peptide Synthesis, Modification and Bioconjugation
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卷首文章：全氟芳基和全氟杂芳基试剂作为肽合成、修饰和生物共轭的新兴工具
DOI：
10.1002/chem.202280762
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发表时间：
2022
期刊：
影响因子：
--
通讯作者：
Brittain W
中科院分区：
文献类型：
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作者：
Brittain W
全氟芳香族化合物和杂芳香族化合物是氨基酸、肽和蛋白质改性的通用试剂。这主要是因为它们与生物亲核试剂进行快速和选择性的亲核取代反应。因此，它们是令人兴奋的工具，在药物发现中调节天然和合成生物分子的生物活性和药物样性质，并在化学生物学研究中添加荧光探针。在这篇迷你评论中，Will Brittain和Chris Coxon调查了当前的领域，讨论了全氟（杂）芳烃的合成，其物理和化学性质带来的挑战，如何克服这些挑战，以及这些重要的新工具的未来。有关更多信息，请参见第10页的小审查。
Perfluorinated aromatics and heteroaromatics are versatile reagents for the modification of amino acids, peptides and proteins. This is principally because they undergo rapid and selective nucleophilic substitution reactions with biological nucleophiles. They are, therefore, exciting tools with which to modulate the biological activities and drug-like properties of natural and synthetic biomolecules in drug discovery and with which to append, for example, fluorescent probes in chemical biology studies. In this Minireview, Will Brittain and Chris Coxon survey the current field, discussing the synthetic incorporation of perfluoro (hetero) aromatics, the challenges posed by their physical and chemical properties, how these can be overcome, and what the future holds for these important new tools. For more information, see the Minireview on page 10.