Department of Nuclear Medicine, Shanghai Jiao Tong University Affiliated Sixth People's Hospital, Shanghai, China.
Department of Radiology, University of Wisconsin-Madison, Wisconsin.
Mol Cancer Ther. 2018 Aug;17(8):1625-1636. doi: 10.1158/1535-7163.MCT-18-0087.
Overexpression and/or mutations of the receptor tyrosine kinase (RTK) subfamilies, such as epidermal growth factor receptors (EGFR) and vascular endothelial growth factor receptors (VEGFR), are closely associated with tumor cell growth, differentiation, proliferation, apoptosis, and cellular invasiveness. Monoclonal antibodies (mAb) and tyrosine kinase inhibitors (TKI) specifically inhibiting these RTKs have shown remarkable success in improving patient survival in many cancer types. However, poor response and even drug resistance inevitably occur. In this setting, the ability to detect and visualize RTKs with noninvasive diagnostic tools will greatly refine clinical treatment strategies for cancer patients, facilitate precise response prediction, and improve drug development. Positron emission tomography (PET) agents using targeted radioactively labeled antibodies have been developed to visualize tumor RTKs and are changing clinical decisions for certain cancer types. In the present review, we primarily focus on PET imaging of RTKs using radiolabeled antibodies with an emphasis on the clinical applications of these immunoPET probes. .
受体酪氨酸激酶 (RTK) 亚家族的过度表达和/或突变,如表皮生长因子受体 (EGFR) 和血管内皮生长因子受体 (VEGFR),与肿瘤细胞的生长、分化、增殖、凋亡和细胞侵袭密切相关。特异性抑制这些 RTKs 的单克隆抗体 (mAb) 和酪氨酸激酶抑制剂 (TKI) 在改善许多癌症类型患者的生存方面取得了显著成功。然而,不可避免地会出现反应不佳甚至耐药的情况。在这种情况下,能够使用非侵入性诊断工具检测和可视化 RTKs,将极大地完善癌症患者的临床治疗策略,促进精确的反应预测,并改善药物开发。使用靶向放射性标记抗体的正电子发射断层扫描 (PET) 剂已被开发用于可视化肿瘤 RTKs,并正在改变某些癌症类型的临床决策。在本综述中,我们主要侧重于使用放射性标记抗体进行 RTK 的 PET 成像,并重点介绍这些免疫 PET 探针的临床应用。