2022年诺贝尔化学奖授予了研究点击化学的科学家，药剂学版块刚开通，那我也发帖捧一下场，搬运一篇将点击化学应用于连接配体与脂质体的论文。
论文链接：
Coupling of Ligands to the Liposome Surface by Click Chemistry
机翻摘要：
点击化学代表了一种新的生物结合策略，可用于方便地将各种配体连接到预先形成的脂质体的表面。这种高效和化学选择性的反应涉及到Cu(I)催化的叠氮-烷基环化反应，可以在水介质中的温和实验条件下进行。在这里，我们描述了一个模型点击反应的应用，在一个单一步骤中，将未受保护的α-1-硫代甘露糖配体，用一个叠氮基团功能化，与含有终端烷基功能化脂质锚的脂质体进行连接。在bathophenanthroline二磺酸盐（一种水溶性铜离子螯合剂）作为催化剂的情况下，获得了极好的偶联产量。这种共轭反应没有引发囊泡的泄漏，而且耦合的甘露糖配体暴露在脂质体的表面。Cu(I)催化的点击反应的主要限制是，这种共轭反应仅限于由饱和（磷脂）脂质构成的脂质体。为了规避这一限制，我们开发了一个替代性的无铜叠氮-烯点击反应的例子。这里介绍了分子工具和结果。
摘要原文：
Click chemistry represents a new bioconjugation strategy that can be used to conveniently attach various ligands to the surface of preformed liposomes. This efficient and chemoselective reaction involves a Cu(I)-catalyzed azide-alkyne cycloaddition which can be performed under mild experimental conditions in aqueous media. Here we describe the application of a model click reaction to the conjugation, in a single step, of unprotected α-1-thiomannosyl ligands, functionalized with an azide group, to liposomes containing a terminal alkyne-functionalized lipid anchor. Excellent coupling yields have been obtained in the presence of bathophenanthroline disulfonate, a water soluble copper-ion chelator, acting as a catalyst. No vesicle leakage is triggered by this conjugation reaction and the coupled mannose ligands are exposed at the surface of the liposomes. The major limitation of Cu(I)-catalyzed click reactions is that this conjugation is restricted to liposomes made of saturated (phospho)lipids. To circumvent that constraint, an example of alternative copper-free azide-alkyne click reaction has been developed. Molecular tools and results are presented here.