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Dual-Receptor Targeted Imaging of Cancer Cells with a Bioorthogonal Iridium(III)-Based Probe.
Shaozhen Jing1,2, Jia Wu3, Kai Yang4
1Research & Development Institute of Northwestern Polytechnical University in Shenzhen, 45 South Gaoxin Road, Shenzhen 518057, China.
Inorganic Chemistry
|April 6, 2026
Summary
New dual receptor-mediated luminescent iridium(III) complexes offer precise cancer cell imaging. These probes utilize bioorthogonal activation for enhanced specificity in detecting cancer biomarkers like carbonic anhydrase IX (CAIX).
Area of Science:
- Inorganic Chemistry
- Biomedical Imaging
- Chemical Biology
Background:
- Luminescence probes are vital for cancer detection and surgical navigation.
- Current probes targeting single receptors face challenges with specificity and background noise.
- Accurate imaging of cancer cells requires improved probe design.
Purpose of the Study:
- To develop novel dual receptor-mediated luminescent iridium(III) complexes for precise cancer cell imaging.
- To employ a bioorthogonal activation strategy for enhanced probe performance.
- To target carbonic anhydrase IX (CAIX) and biotin receptors for specific cancer cell detection.
Main Methods:
- Design and synthesis of two dual receptor-mediated luminescent iridium(III) complexes.
- Incorporation of benzenesulfonamide for CAIX targeting and BCN-biotin for biotin receptor targeting.
- Evaluation of luminescence enhancement, reaction kinetics, and specificity in cancer cell lines.
Main Results:
- Complexes 1 and 2 showed significant luminescence enhancement (16- and 29-fold) upon bioorthogonal reaction.
- Rapid second-order rate constants (k2) were determined for the probe activation.
- Complex 2 demonstrated sensitive and specific detection of CAIX-overexpressing cancer cells with minimal signal in low-CAIX cells.
Conclusions:
- Dual receptor-mediated iridium(III) complexes with bioorthogonal activation show promise for accurate cancer cell imaging.
- This strategy enhances probe specificity and reduces background interference.
- The developed probes offer a potential advancement in cancer diagnostics and image-guided surgery.
