Click Bioconjugation: Modifying Proteins Using Click‐Like Chemistry

Abstract Bioconjugation deals with the chemical modification of proteins. The reactions used exploit either the intrinsic chemical reactivity of the biomolecule or introduce functionalities that can then be subsequently reacted without interfering with other functional groups of the biological entity. Perfectly selective, high yielding chemical transformations are needed that can be run in aqueous environment under mild pH conditions. Requirements that have an obvious overlap with the definition of click chemistry. This review shows a selection of successfully applied click‐type reactions in bioconjugation as well as some recent developments to broaden the chemical toolbox to meet the challenge of selective, bioorthogonal modification of biomolecules.