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1. (WO2018089951) REDOX-BASED REAGENTS FOR METHIONINE BIOCONJUGATION

Pub. No.:    WO/2018/089951    International Application No.:    PCT/US2017/061412
Publication Date: Fri May 18 01:59:59 CEST 2018 International Filing Date: Tue Nov 14 00:59:59 CET 2017
IPC: A61K 31/33
C07D 273/00
Applicants: REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors: LIN, ShiXian
YANG, XiaoYu
TOSTE, F. Dean
CHANG, Christopher J.
Title: REDOX-BASED REAGENTS FOR METHIONINE BIOCONJUGATION
Abstract:
Chemoselective conjugation is achieved through redox reactivity by reacting an N- transfer oxidant with a thioether substrate in a redox reaction in an aqueous environment to form a conjugation product. In embodiments, Redox-Activated Chemical Tagging (ReACT) strategies for methionine-based protein functionalization. Oxaziridine (Ox) compounds serve as oxidant-mediated reagents for direct functionalization by converting methionine to the corresponding sulfimide conjugation product.