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

17 January 2022, Version 1
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

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.

Keywords

protein-protein interactions
stabilizers
ligand discovery
14-3-3 proteins
dynamic combinatorial chemistry

Supplementary materials

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Description
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supporting data and figures
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supporting data, figures, methods and characterization
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Now Published

Towards identification of protein–protein interaction stabilizers via inhibitory peptide-fragment hybrids using templated fragment ligation [opens in a new tab]
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 [opens in a new tab]

DOI

10.26434/chemrxiv-2022-wr02f
D O I: 10.26434/chemrxiv-2022-wr02f [opens in a new tab]

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

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