Recent advances of thiol-selective bioconjugation reactions

Area of Science:

• Biochemistry and Molecular Biology
• Chemical Biology
• Drug Discovery and Development

Background:

• Proteins are essential biomolecules involved in all cellular processes, exhibiting high specificity.
• Chemoselective protein modification, outside genetic code control, is crucial for research tools and therapeutics.
• Cysteine-selective modification is a key strategy for creating functional protein conjugates.

Purpose of the Study:

• To review recent advancements in chemoselective modification of cysteine residues in peptides, proteins, and antibodies.
• To highlight novel reagents for efficient cysteine conjugation.
• To focus on strategies yielding stable conjugates with pharmaceutical relevance.

Main Methods:

• Literature review of recent scientific publications.
• Analysis of emerging strategies for site-selective protein modification.
• Evaluation of new reagents for cysteine conjugation.

Main Results:

• Identification of new chemoselective strategies for cysteine modification.
• Highlighting novel reagents enabling efficient and stable protein conjugation.
• Demonstrating the pharmaceutical applicability of resulting conjugates.

Conclusions:

• Recent strategies significantly enhance chemoselective cysteine modification.
• New reagents facilitate the development of protein-based therapeutics.
• Cysteine conjugation remains a powerful tool for biological exploration and drug development.