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

Autor:	Watson, Morag E., Scott, Daniel, Jamieson, Craig, Layfield, Robert, Mason, Andrew M.
Předmět:	PEPTIDES UBIQUITIN PROTEIN-protein interactions ALZHEIMER'S disease
Zdroj:	Peptide Science; Jan2021, Vol. 113 Issue 1, p1-12, 12p
Abstrakt:	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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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