Chemical modification of protein is an arduous but fruitful task. Many chemical methods have been developed for such purpose by carefully balancing reactivity and selectivity. Now both chemists and biologists have in hand an arsenal of tools from which they can select a relevant reaction to tackle their problems. This review focuses on the various chemical transformations available for selective modification of proteins. It also provides a brief overview of some of their main applications, including detection of protein interactions, preparation of bioconjugates, and protein microarrays.

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