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The discovery of effective therapies against antibiotic\u2010resistant pathogens has become an urgent need, necessitating innovative approaches to accelerate the identification and development of novel antibacterial agents. On the other hand, the expression of the \u03b2\u2010lactam\u2010hydrolyzing enzyme (\u03b2\u2010lactamase), the major cause of bacterial resistance to \u03b2\u2010lactam antibiotics, provides a distinctive opportunity to visualize bacterial infection, evaluate the efficacy of existing antibiotics, screen for novel antibacterial agents, and optimize drug dosing regimens in live animals. Herein, a hydrophilicity\u2010switching, self\u2010immobilizing, near\u2010Infrared fluorogenic \u03b2\u2010lactamase probe for the highly sensitive imaging of bacterial infection in live mice is reported. This probe, in addition to a significant increase in fluorescence upon selective hydrolysis by \u03b2\u2010lactamases as conventional \u03b2\u2010lactamase probes, also massively enriches within \u03b2\u2010lactamase\u2010expressing bacteria (over 1500\u2010folds compared to the incubation medium), which renders excellent sensitivity in the imaging of bacterial infections in living animals. This agent has proven to enable the assessment of antibiotic therapeutic efficacy and potency of \u03b2\u2010lactamase inhibitors in living animals in a non\u2010invasive and much more convenient manner.<\/jats:p>","DOI":"10.1002\/advs.202408559","type":"journal-article","created":{"date-parts":[[2024,12,12]],"date-time":"2024-12-12T05:48:05Z","timestamp":1733982485000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["Highly Sensitive In Vivo Imaging of Bacterial Infections with a Hydrophilicity\u2010Switching, Self\u2010Immobilizing, Near\u2010Infrared Fluorogenic \u03b2\u2010Lactamase Probe Enriched within Bacteria"],"prefix":"10.1002","volume":"12","author":[{"given":"Fangfang","family":"Chen","sequence":"first","affiliation":[{"name":"State Key Laboratory of Bioreactor Engineering Shanghai Key Laboratory of New Drug Design Frontiers Science Center for Materiobiology and Dynamic Chemistry Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism School of Pharmacy East China University of Science and Technology  Shanghai 200237 P.R. 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