Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St, Luzhou, Sichuan 646000, China.
Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, No.25, Taiping St, Luzhou, Sichuan 646000, China.
Curr Top Med Chem. 2019;19(1):17-32. doi: 10.2174/1568026619666190201094952.
Malignant tumors are a major cause of death. The lack of methods that provide an early diagnosis and adequate treatment of cancers is the main obstacle to precision medicine. The C-X-C chemokine receptor 4 (CXCR4) is overexpressed in various tumors and plays a key role in tumor pathogenesis. Therefore, CXCR4-targeted molecular imaging can quickly and accurately detect and quantify CXCR4 abnormalities in real time. The expression level and activation status of CXCR4 are very important for screening susceptible populations and providing an accurate diagnosis and optimal treatment. In view of the fact that radionuclide-labeled peptides have become widely used for the diagnosis and treatment of tumors, this manuscript reviews the potential of different radionuclide-labeled peptide inhibitors for the targeted imaging of CXCR4- positive tumors and targeted treatment. The article also discusses the specificity and in vivo distribution of radionuclide-labeled peptide inhibitors, and translation of these inhibitors to the clinic.
恶性肿瘤是导致死亡的主要原因之一。缺乏能够提供早期诊断和充分治疗癌症的方法是精准医学的主要障碍。C-X-C 趋化因子受体 4（CXCR4）在各种肿瘤中过度表达，在肿瘤发病机制中起关键作用。因此，CXCR4 靶向分子成像可以快速、准确地实时检测和定量 CXCR4 异常。CXCR4 的表达水平和激活状态对于筛选易感人群以及提供准确的诊断和最佳治疗非常重要。鉴于放射性核素标记肽已广泛用于肿瘤的诊断和治疗，本文综述了不同放射性核素标记肽抑制剂在 CXCR4 阳性肿瘤的靶向成像和靶向治疗中的应用潜力。本文还讨论了放射性核素标记肽抑制剂的特异性和体内分布，以及这些抑制剂向临床的转化。
