Bioorthogonal chemistry: Optimization and application updates during 2013–2017

Abstract Bioorthogonal chemical groups to tag naturally occurring biomolecules in their native setting is a powerful tool for studying and manipulating biological processes, whereby unique functional groups incorporated into target biomolecules can be detected in a second step by using selective partners. On the other hand, bioorthogonal cleavage reactions enables chemically controlled spatiotemporal activation of intracellular proteins and prodrugs. Considerable attention has been focused on the bioorthogonal reactions, not only optimizing the known bioorthogonal reagents to gain fast reaction kinetics, high stability of the reagents and the products, but also extending new applications as well as developing new types of bioorthogonal reactions.