Bioorthogonal Copper‐Free Click Chemistry In Vivo for Tumor‐Targeted Delivery of Nanoparticles

Right on target: An in vivo tumor-targeting strategy using nanoparticles has been developed. An unnatural sialic acid (green, see scheme) with azide groups is artificially generated on the target site by metabolic glycoengineering. These groups then effectively enhance the accumulation of nanoparticles in the target tumor site by an in vivo bioorthogonal copper-free click reaction.