Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford OX1 3TA, UK.
Nat Commun. 2014 Sep 5;5:4740. doi: 10.1038/ncomms5740.
Chemical modification of proteins is an important tool for probing natural systems, creating therapeutic conjugates and generating novel protein constructs. Site-selective reactions require exquisite control over both chemo- and regioselectivity, under ambient, aqueous conditions. There are now various methods for achieving selective modification of both natural and unnatural amino acids--each with merits and limitations--providing a 'toolkit' that until 20 years ago was largely limited to reactions at nucleophilic cysteine and lysine residues. If applied in a biologically benign manner, this chemistry could form the basis of true Synthetic Biology.
蛋白质的化学修饰是研究自然系统、制备治疗性偶联物和构建新型蛋白质结构的重要工具。在温和的水相条件下，实现化学和区域选择性的精确控制对于选择性反应至关重要。目前有多种方法可以实现天然和非天然氨基酸的选择性修饰，每种方法都有其优点和局限性，为 20 年前主要局限于亲核半胱氨酸和赖氨酸残基反应的“工具箱”提供了更多选择。如果以生物相容性的方式应用这种化学方法，它可以为真正的合成生物学奠定基础。
