Bioorthogonal chemistry refers to chemical reactions that can be carried out in biological systems without interfering with natural biochemical processes. During the past two decades since its emergence, the scope of bioorthogonal chemistry has been greatly expanded from ligation to cleavage reactions, with broad applications ranging from live cells to animals for biological studies, medical as well as pharmaceutical research. Chinese chemical biologists have actively participated in this exciting area, and a series of important work has been carried out with notable achievements. In particular, the creation and development of bioorthogonal cleavage reactions and its diverse applications have drawn considerable attentions. In this review, we summarize the representative work on bioorthogonal chemistry that been developed in China in recent five years. These works will be categorized into metal-, photo-and small molecule-mediated bioorthogonal ligation as well as cleavage reactions, respectively. In the end, we will discuss the future development along this exciting avenue and the further innovation of the "remote-control bioorthogonal chemistry", which may eventually drive the bioorthogonal reactions into living animals or even human being.

No abstract