Background: Cu-catalyzed azide–alkyne cycloaddition (CuAAC), as the most exemplary click reaction,
plays an important role in attaching a probe or substrate of interest to a specific bio-macromolecule or
small molecule. So CuAAC has attracted many chemists and biologists interest.
Objective: Click reaction provides a powerful tool to solve tremendous questions in chemical biology. Using
CuAAC, chemists and biologists dug into plentiful chemical and biological problems.
Conclusion: This review focuses on the CuAAC and its recent applications in different fields. The applications
of CuAAC are dispersing to the field of detecting hydrazoic acids, fluoride ions, and labeling proteins, nucleic
acids or other biological molecules and even in material science. Both in small molecular and biological macromolecular
detection, CuAAC plays an important role and provides a lot of methods to investigate biological
processes. The promoted CuAAC reaction is studied well and the applications of CuAAC in solid phase synthesis
are described. In addition, more applications of CuAAC can be developed.