journal article·2025-05Open access

An Intracellular Peptide Library Screening Platform Identifies Irreversible Covalent Transcription Factor Inhibitors (Adv. Sci. 18/2025)

Andrew Brennan, Scott Lovell, Keith W Vance, Jody M Mason

Advanced Science· Volume 12· Issue 18

Abstract

Covalent Peptide Library Screening Platform A peptide library screening platform was developed to discover covalent transcription factor inhibitors. It identified an antagonist cysteine residue which formed a inhibitory disulphide with cJun C269. Cysteine conversion to an electrophile generated an irreversible and selective cJun inhibitor, validating the approach for covalent antagonist discovery. More details can be found in article number 2416963 by Jody M. Mason and co-workers. Image credit: Jaiveer Arora.
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OpenAlex topics: Click Chemistry and Applications

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