Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Student Research Committee, Mazandaran University of Medical Sciences, Sari, Iran.
Chem Biol Drug Des. 2019 Mar;93(3):205-221. doi: 10.1111/cbdd.13413. Epub 2018 Oct 30.
Targeting overexpressed receptors on the cancer cells with radiolabeled peptides has become very important in nuclear oncology in the recent years. Peptides are small and have easy preparation and easy radiolabeling protocol with no side-effect and toxicity. These properties made them a valuable tool for tumor targeting. Based on the successful imaging of neuroendocrine tumors with In-octreotide, other receptor-targeting peptides such as bombesin (BBN), cholecystokinin/gastrin analogues, neurotensin analogues, glucagon-like peptide-1, and RGD peptides are currently under development or undergoing clinical trials. The most frequently used radionuclides for tumor imaging are Tc and In for single-photon emission computed tomography and Ga and F for positron emission tomography imaging. This review presents some of the Tc-labeled peptides, with regard to their potential for radionuclide imaging of tumors in clinical and preclinical application.
近年来，用放射性核素标记的肽靶向癌细胞过度表达的受体在核医学中变得非常重要。肽体积小，制备简单，放射性标记方案简单，无副作用和毒性。这些特性使它们成为肿瘤靶向的有价值的工具。基于 In-octreotide 对神经内分泌肿瘤的成功成像，其他受体靶向肽，如 bombesin（BBN）、胆囊收缩素/胃泌素类似物、神经降压素类似物、胰高血糖素样肽-1 和 RGD 肽，目前正在开发或正在进行临床试验。最常用于肿瘤成像的放射性核素是 Tc 和用于单光子发射计算机断层扫描的 In，以及用于正电子发射断层扫描成像的 Ga 和 F。本文综述了一些 Tc 标记的肽，就其在临床和临床前应用中对肿瘤进行放射性核素成像的潜力进行了讨论。
