Fluorogenic Probes/Inhibitors of β-Lactamase and their Applications in Drug-Resistant Bacteria

beta-Lactam antibiotics are generally perceived as one of the greatest inventions of the 20(th) century, and these small molecular compounds have saved millions of lives. However, upon clinical application of antibiotics, the beta-lactamase secreted by pathogenic bacteria can lead to the gradual development of drug resistance. beta-Lactamase is a hydrolase that can efficiently hydrolyze and destroy beta-lactam antibiotics. It develops and spreads rapidly in pathogens, and the drug-resistant bacteria pose a severe threat to human health and development. As a result, detecting and inhibiting the activities of beta-lactamase are of great value for the rational use of antibiotics and the treatment of infectious diseases. At present, many specific detection methods and inhibitors of beta-lactamase have been developed and applied in clinical practice. In this Minireview, we describe the resistance mechanism of bacteria producing beta-lactamase and further summarize the fluorogenic probes, inhibitors of beta-lactamase, and their applications in the treatment of infectious diseases. It may be valuable to design fluorogenic probes with improved selectivity, sensitivity, and effectiveness to further identify the inhibitors for beta-lactamases and eventually overcome bacterial resistance.

Automated summary

Beta-lactam antibiotics are important inventions in treating infections, but the emergence of beta-lactamase in bacteria leads to drug resistance. Various detection methods and inhibitors are available, and designing improved probes may help overcome bacterial resistance.