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High Throughput, Real-time, Dual-readout Testing of Intracellular Antimicrobial Activity and Eukaryotic Cell Cytotoxicity
Published on: November 16, 2016
Target engagement in bacterial and protozoan pathogens: in vitro and cellular assays for drug discovery
Priscila Z Ramos1, Carolina M C Catta-Preta2, Rafael M Couñago3
1Centro de Química Medicinal (CQMED), Centro de Biologia Molecular e Engenharia Genética (CBMEG), Universidade Estadual de Campinas, UNICAMP, 13083-886, Campinas, SP, Brazil.
Abstract:
Target engagement (TE) assays are essential for confirming on-target activity, guiding medicinal chemistry, and linking molecular interactions to phenotypic outcomes. Despite their success in human drug discovery, their application to bacterial and protozoan pathogens remains limited due to biological complexity, technical barriers, and lack of high-quality chemical tools and protein reagents. This review surveys current TE strategies and highlights emerging tools such as live-cell bioluminescence resonance energy transfer, cellular thermal shif assay, and chemoproteomics. Expanding TE in pathogen research will deepen mechanistic insights, reduce development risk, and improve the chances of delivering safer, more effective anti-infective therapies.
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