Bioorthogonal Chemistry

Bioorthogonal Chemistry (생체직교성화학 연구)

Bioorthogonal chemistry has emerged over the past few decades as a transformative tool in chemical biology and related disciplines. In recognition of its impact, the 2022 Nobel Prize in Chemistry was awarded to pioneering researchers in this field. Organic reactions once believed to be feasible only in flasks or organic solvents are now possible under complex biological conditions. These new-to-nature bioorthogonal reactions can proceed in living systems—such as cells and animals—without interfering with native biomolecules.

Unlike natural enzymes, bioorthogonal catalysts are engineered to perform abiotic chemical reactions within biological environments. These catalysts can accept and convert unnatural substrates into functional products without disrupting endogenous biological processes. Acting as nanoscale drug factories, bioorthogonal catalysts can locally activate molecules in situ. For example, a non-fluorescent molecule may be transformed into an imaging agent only after entering a target cell, or an inactive prodrug may be converted into its active form exclusively within cancerous tissues.

Thus, bioorthogonal catalysis has become a powerful and practical strategy for generating functional molecules directly inside living organisms—enabling precise therapeutic and diagnostic applications with minimal biological disturbance.

Key publications

• J. Med. Chem. 2025, 68, 15695-15710. doi: 10.1021/acs.jmedchem.5c00696

• Chem. Soc. Rev. 2021, 50, 13467-13480. doi: 10.1039/D0CS00659A 

• Reactions 2024, 5, 231-245. doi: 10.3390/reactions5010010