Heo Dan, Ku Minhee, Kim Jung-Hoon, Yang Jaemoon, Suh Jin-Suck
Department of Radiology, Yonsei University College of Medicine, Seoul, 03722, Republic of Korea.
Systems Molecular Radiology at Yonsei, Seoul, 03722, Republic of Korea.
Nanoscale Res Lett. 2018 Sep 18;13(1):288. doi: 10.1186/s11671-018-2682-3.
The aim of this study was the development of a human epidermal growth factor receptor 2 (HER2)-targetable contrast agent for magnetic resonance imaging (MRI) with a high magnetic sensitivity. An anti-HER2 aptamer-modified magnetic nanosensitizer (Apt-MNS) was prepared by conjugation with 5'-thiol-modified aptamers and maleimidylated magnetic nanocrystals (MNCs). The physicochemical characteristics and targeting ability of Apt-MNS were confirmed, and the binding affinity (K) onto HER2 protein of Apt-MNS was 0.57 ± 0.26 nM. In vivo MRI contrast enhancement ability was also verified at HER2+ cancer cell (NIH3T6.7)-xenograft mouse models (n = 3) at 3T clinical MRI instrument. The control experiment was carried out using non-labeled MNCs. The results indicated that up to 150% contrast enhancement was achieved at the tumor region in the T2-weighted MR images after the injection of the Apt-MNS agent in mice that received the NIH3T6.7 cells.
本研究的目的是开发一种用于磁共振成像（MRI）的、具有高磁敏感性的可靶向人表皮生长因子受体2（HER2）的造影剂。通过将5'-硫醇修饰的适体与马来酰亚胺化的磁性纳米晶体（MNC）偶联，制备了一种抗HER2适体修饰的磁性纳米敏化剂（Apt-MNS）。确认了Apt-MNS的物理化学特性和靶向能力，Apt-MNS与HER2蛋白的结合亲和力（K）为0.57±0.26 nM。还在3T临床MRI仪器上的HER2+癌细胞（NIH3T6.7）异种移植小鼠模型（n = 3）中验证了体内MRI造影增强能力。使用未标记的MNC进行对照实验。结果表明，在接种了NIH3T6.7细胞的小鼠中注射Apt-MNS剂后，T2加权MR图像中肿瘤区域的造影增强高达150%。
