Sun Yao, Zeng Xiaodong, Xiao Yuling, Liu Changhao, Zhu Hua, Zhou Hui, Chen Ziyang, Xu Fuchun, Wang Jule, Zhu Mengyue, Wu Junzhu, Tian Mei, Zhang Hong, Deng Zixin, Cheng Zhen, Hong Xuechuan
State Key Laboratory of Virology , Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals , Wuhan University School of Pharmaceutical Sciences , Wuhan 430071 , China . Email:
Key Laboratory of Pesticides and Chemical Biology , Ministry of Education , College of Chemistry , Central China Normal University , Wuhan 430079 , China.
Chem Sci. 2018 Jan 8;9(8):2092-2097. doi: 10.1039/c7sc04774f. eCollection 2018 Feb 28.
Accurate tumor identification is essential in cancer management. Incomplete excision of tumor tissue, however, negatively affects the prognosis of the patient. To accomplish radical excision of tumor tissue, radiotracers can be used that target tumor tissue and can be detected using a gamma probe during surgery. Intraoperative fluorescence imaging could allow accurate real-time tumor delineation. Herein, a novel dual-modal imaging platform using base-catalyzed double addition of thiols into a propiolamide scaffold has been developed, allowing for the highly efficient and selective assembly of various thiol units in a protecting-group-free manner. The first small-molecule based αvβ-targeted NIR-II/PET probe was concisely generated this strategy and subsequently evaluated in mice bearing the U87MG xenograft. Excellent imaging properties such as good tumor uptake, high tumor contrast and specificity, tumor delineation and image-guided surgery were achieved in the small animal models. These attractive results of allow it to be a promising αvβ-targeted NIR-II/PET probe for clinical translation.
准确的肿瘤识别在癌症治疗中至关重要。然而，肿瘤组织切除不完全会对患者的预后产生负面影响。为了实现肿瘤组织的根治性切除，可以使用靶向肿瘤组织的放射性示踪剂，并在手术期间使用伽马探头进行检测。术中荧光成像可以实现准确的实时肿瘤勾勒。在此，开发了一种新型的双模态成像平台，该平台利用碱催化的硫醇向丙炔酰胺支架的双加成反应，能够以无保护基团的方式高效、选择性地组装各种硫醇单元。基于该策略简洁地制备了首个基于小分子的αvβ靶向近红外二区/正电子发射断层显像（NIR-II/PET）探针，并随后在携带U87MG异种移植瘤的小鼠中进行了评估。在小动物模型中实现了良好的肿瘤摄取、高肿瘤对比度和特异性、肿瘤勾勒以及图像引导手术等优异的成像特性。这些引人注目的结果使其成为一种有前景的用于临床转化的αvβ靶向NIR-II/PET探针。
