2. Academic Validation
  3. Visualizing Tumors in Real Time: A Highly Sensitive PSMA Probe for NIR-II Imaging and Intraoperative Tumor Resection

Visualizing Tumors in Real Time: A Highly Sensitive PSMA Probe for NIR-II Imaging and Intraoperative Tumor Resection

  • J Med Chem. 2021 Jun 10;64(11):7735-7745. doi: 10.1021/acs.jmedchem.1c00444.
Longfei Zhang 1,  Xiaojing Shi 2,  Yuying Li 1,  Xiaojiang Duan 3,  Zeyu Zhang 4,  Hualong Fu 1,  Xing Yang 3,  Jie Tian 2,  Zhenhua Hu 2,  Mengchao Cui 1 5
Affiliations

Affiliations

  • 1 Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
  • 2 CAS Key Laboratory of Molecular Imaging, Beijing Key Laboratory of Molecular Imaging, The State Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing 100190, China.
  • 3 Department of Nuclear Medicine, Peking University First Hospital, Beijing 100034, China.
  • 4 School of Medical Science and Engineering, Beihang University, Beijing 100191, China.
  • 5 Center for Advanced Materials Research, Advanced Institute of Natural Sciences, Beijing Normal University at Zhuhai, Zhuhai 519087, China.
PMID: 34047189 DOI: 10.1021/acs.jmedchem.1c00444
Abstract

Owing to the complex anatomical structure, precise resection of a tumor while maintaining adjacent tissue is a challenge in radical prostatectomy for prostate Cancer (PCa). Optical imaging in near-infrared window II (NIR-II) is a promising technology for intraoperative guidance, whereas there is no available probe for PCa yet. In this article, a novel probe (PSMA-1092) bearing two prostate-specific membrane antigen (PSMA) binding motifs was developed, displaying excellent optical properties (λmax = 1092 nm) and ultrahigh affinity (Ki = 80 pM) toward PSMA. The tumor was visualized with high resolution (tissue-to-normal tissue ratio = 7.62 ± 1.05) and clear margin by NIR-II imaging using PSMA-1092 in a mouse model. During the tumor resection, residual tumors missed by visible inspection were detected by the real-time imaging. Overall, PSMA-1092 displayed excellent performance in delineating the tumor margin and detecting residual tumors, demonstrating promising potential for precise PCa tumor resection in clinical practice.

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