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Design, synthesis and evaluation of E2-25K derived stapled peptides

Watson, Morag E.; Scott, Daniel; Jamieson, Craig; Layfield, Robert; Mason, Andrew M.

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Authors

Morag E. Watson

DANIEL SCOTT DANIEL.SCOTT@NOTTINGHAM.AC.UK
Nottingham Research Fellow

Craig Jamieson

ROBERT LAYFIELD ROBERT.LAYFIELD@NOTTINGHAM.AC.UK
Professor of Protein Biochemistry

Andrew M. Mason



Abstract

© 2020 The Authors. Peptide Science published by Wiley Periodicals, Inc. Stabilised peptides are now established as potential drug candidates to probe previously intractable molecular targets, such as protein-protein interactions. Herein, we report the design and synthesis of eight short helical peptide analogues of the ubiquitin conjugating enzyme, E2-25K, as potential antagonists of the interaction between E2-25K and the Alzheimer's Disease (AD) associated ubiquitin mutant Ubb + 1. Biochemical evaluation revealed four putative antagonists of the Ubb + 1/E2-25K interaction that reduced incorporation of Ubb + 1 into polyubiquitin chains in vitro, validating the potential of this approach as a therapeutic strategy.

Citation

Watson, M. E., Scott, D., Jamieson, C., Layfield, R., & Mason, A. M. (2021). Design, synthesis and evaluation of E2-25K derived stapled peptides. Peptide Science, 113(1), Article e24158. https://doi.org/10.1002/pep2.24158

Journal Article Type Article
Acceptance Date Mar 6, 2020
Online Publication Date Mar 24, 2020
Publication Date 2021-01
Deposit Date Oct 20, 2021
Publicly Available Date Oct 20, 2021
Journal Peptide Science
Electronic ISSN 2475-8817
Publisher Wiley
Peer Reviewed Peer Reviewed
Volume 113
Issue 1
Article Number e24158
DOI https://doi.org/10.1002/pep2.24158
Keywords Organic Chemistry; Biomaterials; Biochemistry; Biophysics
Public URL https://nottingham-repository.worktribe.com/output/5308365
Publisher URL https://onlinelibrary.wiley.com/doi/10.1002/pep2.24158

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