Strain-Promoted Bioorthogonal Chemistry

Abstract

Strain-promoted bioorthogonal reactions, driven by cycloalkynes and cycloalkenes, have become indispensable in chemical biology. These strained chemical tools enable selective bioorthogonal ligations and bond-cleavage reactions, supporting research and development in various emerging fields such as molecular imaging, targeted drug delivery, and biomolecular engineering. The unique reactivities of strained cycloalkynes and cycloalkenes allow for efficient and precise (bio)molecular transformations, even in complex biological environments. This review provides an overview of strain-promoted bioorthogonal reactions, focusing on their mechanisms, kinetics, and other performance characteristics, while emphasizing their critical role in advancing both fundamental research and translational applications.