Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 28, Issue 66, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202201843
Keywords
cysteine bioconjugation; fast kinetics; N-terminal cysteine; protein modification; reaction rate constant
Categories
Funding
- NSF [CHE-1904874/2117246]
- NIH [GM102735/124231]
- Ono Pharma Foundation
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Cysteine bioconjugation plays a crucial role in biological research and has been widely utilized for protein modification, antibody-drug conjugate construction, and cell imaging studies. Recent advancements in fast cysteine bioconjugation have been summarized in this concept, along with discussions on the mechanism and chemical principles that contribute to the high efficiency of newly developed cysteine reactive reagents.
Cysteine bioconjugation serves as a powerful tool in biological research and has been widely used for chemical modification of proteins, constructing antibody-drug conjugates, and enabling cell imaging studies. Cysteine conjugation reactions with fast kinetics and exquisite selectivity have been under heavy pursuit as they would allow clean protein modification with just stoichiometric amounts of reagents, which minimizes side reactions, simplifies purification and broadens functional group tolerance. In this concept, we summarize the recent advances in fast cysteine bioconjugation, and discuss the mechanism and chemical principles that underlie the high efficiencies of the newly developed cysteine reactive reagents.
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