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Single-molecule FRET-based approach for protein-targeted drug discovery.


ABSTRACT: Many therapeutic drugs target various proteins involved in diverse biological processes. Among these proteins, type II topoisomerases are critical targets for anticancer and antibacterial chemotherapies, yet the action mechanisms of many type II topoisomerase-targeting drugs have not been fully elucidated. In this regard, the development of rapid and accurate methods to identify the mode of action of potential drug candidates is crucial to improve the efficiency of drug screening and discovery. Here, using type II topoisomerase as a model system, we present a single-molecule fluorescence resonance energy transfer-based drug screening method capable of delineating when and how the drug candidates participate in the entire reaction steps of the target protein. This unique capability has been

SUBMITTER: Kim Y 

PROVIDER: S-EPMC11667156 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature