Affiliation:
1. Department of Medicine Shizhen College of Guizhou University of Traditional Chinese Medicine Guiyang 550200 China
2. Department of Chemistry Case Western Reserve University Cleveland Ohio 44106 United States
3. State Key Laboratory for Chemo/Biosensing and Chemometrics College of Chemistry and Chemical Engineering Hunan University Changsha 410082 China
4. College of Pharmacy Guizhou University of Traditional Chinese Medicine Guiyang 550025 China
5. Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research College of Chemistry and Chemical Engineering Hunan Normal University Changsha 410081 China
Abstract
AbstractAminopeptidases, enzymes with critical roles in human body, are emerging as vital biomarkers for metabolic processes and diseases. Aberrant aminopeptidase levels are often associated with diseases, particularly cancer. Small‐molecule probes, such as fluorescent, fluorescent/photoacoustics, bioluminescent, and chemiluminescent probes, are essential tools in the study of aminopeptidases‐related diseases. The fluorescent probes provide real‐time insights into protein activities, offering high sensitivity in specific locations, and precise spatiotemporal results. Additionally, photoacoustic probes offer signals that are able to penetrate deeper tissues. Bioluminescent and chemiluminescent probes can enhance in vivo imaging abilities by reducing the background. This comprehensive review is focused on small‐molecule probes that respond to four key aminopeptidases: aminopeptidase N, leucine aminopeptidase, Pyroglutamate aminopeptidase 1, and Prolyl Aminopeptidase, and their utilization in imaging tumors and afflicted regions. In this review, the design strategy of small‐molecule probes, the variety of designs from previous studies, and the opportunities of future bioimaging applications are discussed, serving as a roadmap for future research, sparking innovations in aminopeptidase‐responsive probe development, and enhancing our understanding of these enzymes in disease diagnostics and treatment.