Site-Selective Modification of Biomolecules

Dear Colleagues,

 The site-specific modification of biomolecules plays a central role in chemical biology, helping elucidate definite functions within a complex network of interactions. Furthermore, it has been employed to improve the biological activity and stability of peptides, proteins, carbohydrates, and oligonucleotides. The development of synthetic methodologies and the application of covalent chemical probes are crucial to support these studies. Site-specific labeling can take place on the purified biomolecule, within a cell extract, or even in vivo. Modifications can be introduced via various mechanisms, including bioorthogonal chemistry, (re-)activity-based probes, which utilize electrophiles that modify nucleophiles in, e.g., enzymes, photoaffinity labeling, which makes use of tight-binding inhibitors in combination with a photocrosslinker, metabolic labeling, which utilizes the endogenous metabolic machinery of the cell to introduce site-selective modifications, and site-selective catalysis. This Special Issue aims to draw an overview of the chemical development of the different strategies and their implementation in biological applications.

Prof. Dr. Steven Verhelst
Dr. Martin Witte
Guest Editors

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• activity-based protein profiling
• bioorthogonal chemistry
• click chemistry
• covalent chemical probes
• protein labeling
• photoaffinity labeling
• carbohydrate modification
• oligonucleotide labeling