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Bioorthogonal Molecular Turn-On Optical Imaging and Therapy
Xinzhu Wang1, Donghao Li1, Kanyi Pu1,2
1School of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, Singapore 637457, Singapore.
Chemical Reviews
|January 7, 2026
Summary
Bioorthogonal turn-on optical probes (BioTOPs) enable precise molecular imaging and therapy by activating signals through selective reactions. This technology offers high-contrast visualization and targeted interventions for diagnostics and disease treatment.
Area of Science:
- Chemical Biology
- Molecular Imaging
- Bioorganic Chemistry
Background:
- Bioorthogonal chemistry has advanced molecular imaging and therapy over two decades.
- Bioorthogonal turn-on optical probes (BioTOPs) integrate bioorthogonal handles with imaging agents for signal activation.
- BioTOPs enable high-contrast, real-time visualization of biomolecules and targeted therapy with minimal off-target effects.
Purpose of the Study:
- To review recent advances in the design and application of BioTOPs.
- To discuss the two-step pretargeted strategy for bioorthogonal turn-on optical imaging.
- To categorize bioorthogonal reactions and signal activation mechanisms used in BioTOPs.
Main Methods:
- Categorization of employed bioorthogonal reactions (e.g., Staudinger ligation, cycloadditions, metal-catalyzed reactions).
- Discussion of signal activation mechanisms (e.g., click-to-release, dequenching, decaging, self-assembly).
- Review of design principles for integrating bioorthogonal handles with imaging agents.
Main Results:
- BioTOPs leverage selective bioorthogonal reactions for signal activation, achieving high signal-to-noise ratios.
- Various reaction types and activation mechanisms provide tunable kinetics and high signal turn-on folds.
- The technology facilitates precise spatiotemporal control over optical signal generation.
Conclusions:
- BioTOPs represent a significant innovation for molecular imaging and therapy.
- Applications span biomolecule profiling, cancer diagnosis, and disease-specific interventions.
- This technology holds transformative potential for molecular diagnostics and personalized medicine.
