INTERNATIONAL JOURNAL OF PHARMACEUTICS, cilt.685, 2025 (SCI-Expanded, Scopus)
Bioorthogonal chemistry, referring to chemical reactions that can occur within living systems without interfering with native biological processes, provides a safe and specific method for labeling or linking biomolecules with rapid and efficient reaction kinetics. To date, various bioorthogonal reactions, such as Staudinger Ligation, copper-catalyzed azide-alkyne cycloaddition (CuAAC), copper-free azide-alkyne cycloaddition (SPAAC), and the inverse electron-demand Diels-Alder (IEDDA) reaction, have been developed to achieve improved safety and efficacy. These advanced bioorthogonal reactions have enabled the emergence of innovative treatment strategies for diseases such as cancer, neurodegenerative disorders, ischemia, cardiac hypertrophy, and bacterial infections. Beyond disease treatment, bioorthogonal chemistry has also contributed to the development of advanced diagnostic materials. This review highlights the therapeutic, regenerative, and diagnostic applications of bioorthogonal chemistry.