Specific biomarker-activatable probes have revolutionized theranostics, being beneficial for precision medicine. Hypoxia is a critical pathological characteristic prevalent in numerous major diseases such as cancers, cardiovascular disorders, inflammatory diseases, and acute ischemia. Aggregation-induced emission luminogens (AIEgens) have emerged as a promising tool to tackle the biomedical issues. Of particular significance are the hypoxia-responsive AIEgens, representing a kind of crucial probe capable of delicately sensing and responding to the hypoxic microenvironment, thereby enhancing the precision of disease diagnosis and treatment. In this review, we summarize the recent advances of hypoxia-responsive AIEgens for varied biomedical applications. The hypoxia-responsive structures based on AIEgens, such as azobenzene, nitrobenzene, and N-oxide are presented, which are in response to the reduction property to bring about significant alternations in response spectra and/or fluorescence intensity. The bioapplications including imaging and therapy of tumor and ischemia diseases are discussed. Moreover, the review sheds light on the future challenges and prospects in this field. This review aims to provide comprehensive guidance and understanding into the development of activatable bioprobes, especially the hypoxia-responsive AIEgens for improving the diagnosis and therapy outcome of related diseases.
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