How do you mend inactive tumor suppressor mutants? You glue them!

Summary Protein-protein interactions (PPIs) have emerged as promising yet challenging therapeutic targets. A robust bioassay is required for rapid PPI modulator discovery. Here, we present a time-resolved Förster's (fluorescence) resonance energy transfer assay protocol for PPI modulator screening in a 1536-well plate format. We use hypomorph SMAD4 R361H -SMAD3 PPI as an example to illustrate the application of the protocol for screening of variant-directed PPI inducers. This platform can be readily adapted for the discovery of both small-molecule PPI inducers and inhibitors. For complete details on the use and execution of this protocol, please refer to Tang et al. (2020) .

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A time-resolved fluorescence resonance energy transfer screening assay for discovery of protein-protein interaction modulators

Tang

Niu

Cicka

et al. 2021

STAR Protocols

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How do you mend inactive tumor suppressor mutants? You glue them!

Cited by 1 publication

References 10 publications

A time-resolved fluorescence resonance energy transfer screening assay for discovery of protein-protein interaction modulators

A time-resolved fluorescence resonance energy transfer screening assay for discovery of protein-protein interaction modulators

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