Direct screening of a target-specific covalent binder: stringent regulation of warhead reactivity in a matchmaking environment. Issue 44 (12th May 2021)

• Record Type: Journal Article
• Authors: Tabuchi, Yudai; Watanabe, Takahito; Katsuki, Riku; Ito, Yuji; Taki, Masumi
• Is Part Of: Chemical communications. Volume 57:Issue 44(2021)
• Page Start: 5378
• Page End: 5381
• Publication Date: 2021-05-12
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d1cc01773j
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : To find targeted covalent biologics, we demonstrated a direct screening method of a peptidic covalent binder via reactivity/affinity-based co-selection using T7 phage display. Abstract : A peptide-type covalent binder for a target protein was obtained by direct and stringent screening of a warhead-modified peptide library on the robust T7 phage. The aryl fluorosulfate (fosylate) warhead was activated only in a matchmaking microenvironment created between the target protein and an appropriate peptide during the reactivity/affinity-based co-selection process of extended phage display.