Design, synthesis and evaluation of E2-25K derived stapled peptides
Watson, Morag E. and Scott, Daniel and Jamieson, Craig and Layfield, Robert and Mason, Andrew M. (2020) Design, synthesis and evaluation of E2-25K derived stapled peptides. Peptide Science. e24158. ISSN 1097-0282
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Abstract
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.
ORCID iDs
Watson, Morag E.

Item type: Article ID code: 71917 Dates: DateEvent24 March 2020Published24 March 2020Published Online6 March 2020AcceptedKeywords: Alzheimer disease, ubiquitin, staples, Chemistry, Chemistry(all) Subjects: Science > Chemistry Department: Faculty of Science > Pure and Applied Chemistry
Strategic Research Themes > Health and WellbeingDepositing user: Pure Administrator Date deposited: 27 Mar 2020 15:05 Last modified: 17 Mar 2021 09:23 URI: https://strathprints.strath.ac.uk/id/eprint/71917