Designing Bioorthogonal Reactions for Biomedical Applications
Qingfei Zhang1,2, Gaizhen Kuang1, Li Wang1
1Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou 325001, China.
Research (Washington, D.C.)
|December 18, 2023
Summary
Bioorthogonal reactions enable chemical modifications in living systems without interference. This review covers their development, applications in biomedicine, and future prospects for novel reaction design.
Area of Science:
- Chemical Biology
- Organic Chemistry
Background:
- Bioorthogonal reactions are highly selective chemical transformations that occur within living organisms without disrupting native biochemical processes.
- First proposed in 2003, bioorthogonal chemistry has rapidly advanced as a critical tool in chemical biology.
Purpose of the Study:
- To provide a comprehensive overview of bioorthogonal reactions and their diverse biomedical applications.
- To summarize the current status and future directions of bioorthogonal chemistry.
- To offer guidance for developing new bioorthogonal reactions.
Main Methods:
- Literature review and synthesis of existing research on bioorthogonal reactions.
- Analysis of applications in areas such as bio-labeling, drug discovery, and therapeutic development.
- Discussion of historical development and future trends.
Main Results:
- Bioorthogonal reactions are characterized by high yield, selectivity, and efficiency.
- Key applications include bio-labeling, nucleic acid functionalization, drug discovery, drug activation, antibody-drug conjugate synthesis, and proteolysis-targeting chimera development.
- The field has seen significant growth and innovation since its inception.
Conclusions:
- Bioorthogonal chemistry is a powerful and versatile tool with broad biomedical impact.
- Continued development of novel bioorthogonal reactions is crucial for expanding their utility.
- This review serves as a guide for researchers in the field.


