Bioorthogonal Click Chemistry: Invention to Applications in Living Systems

Soon after that invention of modular ‘CuAAC Click Chemistry’ by two independent group of researchers, Morten Meldal and Karl Barry Sharpless in 2002, Carolyn Bertozzi introduced the term ‘bioorthogonal chemistry’ to represent a series of reactions which involves the chemical ligation that can occur inside the living systems without interfering and/or interacting with native biochemical processes. Notably, such ligation reactions are characterized by their high specificity, rapid kinetics, and biocompatibility. This chapter highlights the emerging applications of bioorthogonal chemistry enabling the labeling and tracking of biomolecules in real time, providing invaluable insights into biological functions that eventually can revolutionized molecular imaging, drug delivery, and therapeutic strategies.