Crystal structure and ligandability of the 14-3-3/pyrin interface

The identification of chemical starting points for the development of molecular glues is challenging. Here, we employed fragment screening and identified an allosteric stabilizer of the complex between 14−3−3 and a TAZ-derived peptide. The fragment binds preferentially to the 14−3−3/TAZ peptide complex and shows moderate stabilization in differential scanning fluorimetry and microscale thermophoresis. The binding site of the fragment was predicted by molecular dynamics calculations to be distant from the 14−3−3/TAZ peptide interface, located between helices 8 and 9 of the 14−3−3 protein. This site was confirmed by nuclear magnetic resonance and X-ray protein crystallography, revealing the first example of an allosteric stabilizer for 14−3−3 protein−protein interactions.

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The Impact of NLRP3 Inflammasome on Osteoblasts and Osteogenic Differentiation: A Literature Review

Yang,

Xu,

Kang

et al. 2024

JIR

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Crystal structure and ligandability of the 14-3-3/pyrin interface

Cited by 3 publications

References 53 publications

Harnessing the 14-3-3 protein–protein interaction network

Harnessing the 14-3-3 protein–protein interaction network

Fragment-Based Interrogation of the 14–3–3/TAZ Protein–Protein Interaction

The Impact of NLRP3 Inflammasome on Osteoblasts and Osteogenic Differentiation: A Literature Review

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