Staudinger Ligation and Reactions – From Bioorthogonal Labeling to Next‐Generation Biopharmaceuticals

In this review, we highlight groundbreaking discoveries and applications of Staudinger reactions in the molecular life sciences, starting from engineering ligation as a bioorthogonal reaction until most recent modern bioconjugation methods to generate next-generation biopharmaceuticals. Bioorthogonal refer set chemoselective transformations biological environments able take place presence naturally occurring functional groups. The new paradigm such transformations, resulting development various labeling strategies for modification (bio-)molecules interest.