点击化学及其在生物医学领域的应用

"Click Chemistry" and Its Growing Applications in Biomedical Field

自点击化学的概念被Sharpless提出至今,这种模块化、高效和多样性的化学反应在合成化学中得到了广泛应用。Cu(Ⅰ)催化的环加成点击反应被认为是点击化学的精髓。该反应具有区域选择性和化学选择性,并且能够在室温或生理温度下的水介质中进行,因此点击化学近来成为生物和医学领域中最广泛使用的连接工具。本文简要介绍了点击化学的基本概念、反应机理及其优点,重点综述了其在药物开发、聚合物生物缀合物、水凝胶和微凝胶、纳米粒子、微阵列和自组装单分子等生物医学领域的应用,最后总结了目前点击化学存在的主要问题。

The ＂click＂ concept, introduced by Sharpless and coworkers in 2001, is undeniably one of the most important trends in contemporary chemistry. The copper（I）-catalyzed click cycloaddition is generally regarded as the quintessential example of click chemistry, because it can proceeds well in aqueous medium and therefore may be efficiently performed under physiological conditions. Moreover, it holds great chemoselectivity and can therefore be used for modifying highly functional biomolecules such as poly-peptides, nucleic acids or polysaccharides. This mini-review will focus on the recent developments appearing within the literature concerning the application of the click chemistry in drug design, bioconjugation, biomaterials, colloids and planar surfaces.