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- W4283713172 abstract "The development of protein-protein interaction (PPI) inhibitors has been a successful strategy in drug development. However, the identification of PPI stabilizers has proven much more challenging. Here we report a fragment-based drug screening approach using the regulatory hub-protein 14-3-3 as a platform for identifying PPI stabilizers. A homogenous time-resolved FRET assay was used to monitor stabilization of 14-3-3/peptide binding using the known interaction partner estrogen receptor alpha. Screening of an in-house fragment library identified fragment 2 (VUF15640) as a putative PPI stabilizer capable of cooperatively stabilizing 14-3-3 PPIs in a cooperative fashion with Fusicoccin-A. Mechanistically, fragment 2 appears to enhance 14-3-3 dimerization leading to increased client-protein binding. Functionally, fragment 2 enhanced potency of 14-3-3 in a cell-free system inhibiting the enzyme activity of the nitrate reductase. In conclusion, we identified a general PPI stabilizer targeting 14-3-3, which could be used as a tool compound for investigating 14-3-3 client protein interactions." @default.
- W4283713172 created "2022-06-30" @default.
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- W4283713172 date "2022-07-19" @default.
- W4283713172 modified "2023-10-18" @default.
- W4283713172 title "Fragment Screening Yields a Small‐Molecule Stabilizer of 14‐3‐3 Dimers That Modulates Client Protein Interactions" @default.
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- W4283713172 doi "https://doi.org/10.1002/cbic.202200178" @default.
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