Towards Identification of Protein-Protein Interaction Stabilizers via Inhibitory Peptide-Fragment Hybrids Using Templated Fragment Ligation

Sonja  Srdanovic; Zsofia Hegedus; Stuart Warriner; Wilson Andrew

doi:10.26434/chemrxiv-2022-wr02f

Working Paper

Abstract

Using the hDMX/14-3-3 interaction, acylhydrazone-based ligand-directed fragment ligation was used to identify protein-protein interaction (PPI) inhibitory peptide-fragment hybrids. Separation of the peptide-fragment hybrids into the components yielded fragments that stabilized the hDMX/14-3-3 interaction.

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Supplementary material

supporting data and figures

supporting data, figures, methods and characterization

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Towards identification of protein–protein interaction stabilizers via inhibitory peptide-fragment hybrids using templated fragment ligation

Sonja Srdanović, Zsofia Hegedüs, Stuart L. Warriner, Andrew J. Wilson journal article

RSC Chemical Biology , Volume 3, Issue 5

Online publication date: 2022

Version History

Jan 17, 2022 Version 1

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The content is available under CC BY 4.0 License CreativeCommons.org

DOI

10.26434/chemrxiv-2022-wr02f

Funding

Engineering and Physical Sciences Research Council

EP/N013573/1

Engineering and Physical Sciences Research Council

EP/KO39292/1

Horizon 2020 Framework Programme

675179

Author’s competing interest statement

The author(s) have declared they have no conflict of interest with regard to this content

Ethics

The author(s) have declared ethics committee/IRB approval is not relevant to this content

Keywords

protein-protein interactions

stabilizers

ligand discovery

14-3-3 proteins

dynamic combinatorial chemistry

Publication

This content is an early or alternative research output and has not been peer-reviewed at the time of posting.