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Peer-reviewedCC BY-NCRSC advances

A GRPR-targeted near-infrared fluorescent probe for precise tumor imaging and intraoperative surgical navigation

  • Huihui Lu1,2
  • Caiting Deng2,3
  • Jiayao Zhao2
  • Jingjing Zhang2
  • Anping Cao2
  • Feifei An2,4
  • Nandi Chen5
  • Yichao Chai1
5 affiliations
  1. 1The Comprehensive Breast Care Center, The Second Affiliated Hospital of Xi'an Jiaotong University No. 157 Xiwu Road Xi'an Shaanxi 710004 China
  2. 2School of Public Health, Health Science Center, Xi'an Jiaotong University No. 76 Yanta West Road Xi'an 710061 Shaanxi China
  3. 3Institute of Medical Engineering, School of Basic Medical Science, Health Science Center, Xi'an Jiaotong University No. 76 Yanta West Road Xi'an 710061 Shaanxi China
  4. 4State Key Laboratory of Molecular Engineering of Polymers (Fudan University) Shanghai 200438 China
  5. 5Analysis and Testing Center, Shenzhen Technology University Shenzhen Guangdong 518118 China
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Abstract

Fluorescence-guided surgery requires tumor-imaging probes that provide reliable contrast while minimizing background interference. Herein, we developed a gastrin-releasing peptide receptor (GRPR)-targeted near-infrared (NIR) fluorescent probe, IR783-BBN, by covalently conjugating the bombesin peptide with the IR783 fluorophore. This molecular design was intended to combine the tumor-targeting potential of bombesin (BBN) with the NIR imaging capability of IR783. IR783-BBN was successfully synthesized and exhibited absorption and emission maxima at 801 and 820 nm, respectively. In vitro studies demonstrated that the probe cell viability remained above 82% under the tested conditions and was internalized by 4T1 breast cancer cells in a time- and concentration-dependent manner. In 4T1 tumor-bearing mice, IR783-BBN generated detectable tumor-associated fluorescence after systemic administration, with a tumor-to-muscle fluorescence ratio of 6.97 at 1 h post-injection (n = 3). Histological and fluorescence microscopic analyses of the excised tissues further supported the correspondence between fluorescence signals and tumor-containing specimens. Overall, these findings support the feasibility of IR783-BBN as a BBN-conjugated NIR fluorescent probe for tumor imaging and fluorescence-guided surgical navigation.

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Cite

BibTeXRIS
BibTeX
@article{lu2026grprtargeted,
  title = {{A GRPR-targeted near-infrared fluorescent probe for precise tumor imaging and intraoperative surgical navigation}},
  author = {Huihui Lu and Caiting Deng and Jiayao Zhao and Jingjing Zhang and Anping Cao and Feifei An and Nandi Chen and Yichao Chai},
  journal = {RSC advances},
  year = {2026},
  month = oct,
  doi = {10.1039/d6ra06275j},
  url = {https://europepmc.org/article/PMC/PMC13721913},
  note = {CC BY-NC},
}
RIS
TY  - JOUR
TI  - A GRPR-targeted near-infrared fluorescent probe for precise tumor imaging and intraoperative surgical navigation
AU  - Huihui Lu
AU  - Caiting Deng
AU  - Jiayao Zhao
AU  - Jingjing Zhang
AU  - Anping Cao
AU  - Feifei An
AU  - Nandi Chen
AU  - Yichao Chai
PY  - 2026
DA  - 2026/10/30
JO  - RSC advances
DO  - 10.1039/d6ra06275j
UR  - https://europepmc.org/article/PMC/PMC13721913
AB  - Fluorescence-guided surgery requires tumor-imaging probes that provide reliable contrast while minimizing background interference. Herein, we developed a gastrin-releasing peptide receptor (GRPR)-targeted near-infrared (NIR) fluorescent probe, IR783-BBN, by covalently conjugating the bombesin peptide with the IR783 fluorophore. This molecular design was intended to combine the tumor-targeting potential of bombesin (BBN) with the NIR imaging capability of IR783. IR783-BBN was successfully synthesized and exhibited absorption and emission maxima at 801 and 820 nm, respectively. In vitro studies demonstrated that the probe cell viability remained above 82% under the tested conditions and was internalized by 4T1 breast cancer cells in a time- and concentration-dependent manner. In 4T1 tumor-bearing mice, IR783-BBN generated detectable tumor-associated fluorescence after systemic administration, with a tumor-to-muscle fluorescence ratio of 6.97 at 1 h post-injection (n = 3). Histological and fluorescence microscopic analyses of the excised tissues further supported the correspondence between fluorescence signals and tumor-containing specimens. Overall, these findings support the feasibility of IR783-BBN as a BBN-conjugated NIR fluorescent probe for tumor imaging and fluorescence-guided surgical navigation.
SN  - 2046-2069
ER  -