Zhang Longfei, Shi Xiaojing, Li Yuying, Duan Xiaojiang, Zhang Zeyu, Fu Hualong, Yang Xing, Tian Jie, Hu Zhenhua, Cui Mengchao
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
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.
J Med Chem. 2021 Jun 10;64(11):7735-7745. doi: 10.1021/acs.jmedchem.1c00444. Epub 2021 May 28.
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 () bearing two prostate-specific membrane antigen (PSMA) binding motifs was developed, displaying excellent optical properties (λ = 1092 nm) and ultrahigh affinity ( = 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 in a mouse model. During the tumor resection, residual tumors missed by visible inspection were detected by the real-time imaging. Overall, displayed excellent performance in delineating the tumor margin and detecting residual tumors, demonstrating promising potential for precise PCa tumor resection in clinical practice.
由于解剖结构复杂，在前列腺癌（PCa）根治性前列腺切除术中，在保留相邻组织的同时精确切除肿瘤是一项挑战。近红外二区（NIR-II）光学成像技术是一种很有前景的术中引导技术，然而目前尚无用于PCa的探针。在本文中，我们开发了一种新型探针（），其带有两个前列腺特异性膜抗原（PSMA）结合基序，对PSMA显示出优异的光学性质（λ = 1092 nm）和超高亲和力（ = 80 pM）。在小鼠模型中，使用该探针通过NIR-II成像以高分辨率（组织与正常组织比率 = 7.62 ± 1.05）和清晰边界对肿瘤进行了可视化。在肿瘤切除过程中，通过实时成像检测到肉眼检查遗漏的残留肿瘤。总体而言，该探针在勾勒肿瘤边界和检测残留肿瘤方面表现出优异性能，在临床实践中进行精确PCa肿瘤切除方面显示出有前景的潜力。
