Recent years have seen a dramatic expansion of the number of chemical techniques that can be used to achieve site-selective protein modification. These reactions have been developed to work in aqueous media under mild pH and temperature conditions, and can achieve exquisitely high levels of chemoselectivity. This presentation will describe several new oxidative strategies for protein modification that are based on the addition of anilines to electron-rich aromatic species under mild oxidizing conditions. These reactions occur with very high efficiency, and are particularly useful for radiolabeling and the site-specific coupling of full-sized biomolecules. The use of these techniques to prepare complex, multifunctional bioconjugates for drug delivery and diagnostic imaging applications will also be presented.

Oxidative strategies for site-selective protein modification

245th National Meeting (2013)

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