Click Chemistry and Bioorthogonal Reaction for Aggregation‐Induced Emission Bioconjugates

ABSTRACT The resulting product of biocoupling is a bioconjugate, typically formed by linking molecules to proteins, oligosaccharides, nucleic acids, or synthetic polymers. By conjugating fluorescent probes with bioactive molecules via click chemistry or bioorthogonal reaction, functional materials with high specificity, sensitivity, and accuracy can be developed. A particularly promising strategy involves the use of aggregation‐induced emission (AIE) fluorophores, which exhibit augmented luminescence intensity and excellent photostability when in the aggregated state, making them especially suitable for bioimaging and biosensing applications. The rapid expansion of AIE active bioconjugates now calls for a comprehensive review to summarize and systematize recent advances. In this review, we direct our focus toward the biosensing, bioimaging, and therapeutic applications of AIE active bioconjugates prepared via click chemistry or bioorthogonal reactions. We anticipate that this overview will promote the development of versatile AIE bioconjugates and inspire further innovations in bioorthogonal chemistry for biomedical applications.