基于Dar衍生物的前列腺癌grpr靶向PET探针的设计与合成

IF 4.6 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Xiangning Luo BS , Renli Luo MS , Yuanyuan Zhou BS , Yuanpeng Jiang BS , Cong Han BS , Aiguo Song PhD , Kun Qian PhD , Chunrong Qu PhD , Rui Cao PhD , Bin Xu PhD , Zhen Cheng PhD
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引用次数: 0

摘要

胃泌素释放肽受体(GRPR)在大多数前列腺癌(PCa)中过表达,是诊断和治疗的潜在靶点。本研究以已有报道的GRPR拮抗剂RM26和新型螯合剂Dar衍生物为基础,设计并评价了[68Ga]Ga-Dar-C5-P2-RM26和[68Ga]Ga-Dar-P2-RM26两种放射性药物。两种示踪剂均易于室温制备,在磷酸盐缓冲盐水(PBS)和胎牛血清(FBS)中表现出较高的放射化学稳定性。细胞和动物实验表明,这两种放射性示踪剂在PC-3异种移植小鼠模型中表现出特异性的肿瘤摄取。其中,[68Ga]Ga-Dar-C5-P2-RM26和[68Ga]Ga-Dar-P2-RM26的肿瘤摄取率分别为6.617±0.245%和5.973±1.261%。正电子发射断层扫描/计算机断层扫描(PET/CT)成像结果显示,这两种放射性示踪剂在静脉注射(p.i)后0.5小时、1小时和2小时显示出良好的肿瘤-背景对比。综上所述,[68Ga]Ga-Dar-C5-RM26和[68Ga]Ga-Dar-RM26是grpr靶向的放射性示踪剂,在肿瘤靶向成像中具有很高的临床转化潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer

Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer
Gastrin-releasing peptide receptor (GRPR) is overexpressed in most prostate cancers (PCa) and is a potential target in diagnosis and treatment. In this study, based on the previously reported GRPR antagonist RM26 and novel chelating agent Dar derivatives, we designed and evaluated two radiopharmaceuticals, [68Ga]Ga-Dar-C5-P2-RM26 and [68Ga]Ga-Dar-P2-RM26. Both radiotracers were easily prepared at room temperature and showed high radiochemical stability in phosphate-buffered saline (PBS) and fetal bovine serum (FBS). Cellular and animal experiments indicated that the two radiotracers exhibited specific tumor uptakes in PC-3 xenograft mice models. Specifically, [68Ga]Ga-Dar-C5-P2-RM26 and [68Ga]Ga-Dar-P2-RM26 displayed 6.617 ± 0.245 % ID/g and 5.973 ± 1.261 % ID/g tumor uptake, respectively. Positron emission tomography/ computer tomography (PET/CT) imaging results indicated that these two radiotracers showed excellent tumor-to-background contrast at 0.5 h, 1 h, and 2 h post intravenous injection (p.i.). In summary, [68Ga]Ga-Dar-C5-RM26 and [68Ga]Ga-Dar-RM26 are GRPR-targeted radiotracers with high potential for clinical translation in tumor-targeted imaging.
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来源期刊
CiteScore
11.10
自引率
0.00%
发文量
133
审稿时长
42 days
期刊介绍: The mission of Nanomedicine: Nanotechnology, Biology, and Medicine (Nanomedicine: NBM) is to promote the emerging interdisciplinary field of nanomedicine. Nanomedicine: NBM is an international, peer-reviewed journal presenting novel, significant, and interdisciplinary theoretical and experimental results related to nanoscience and nanotechnology in the life and health sciences. Content includes basic, translational, and clinical research addressing diagnosis, treatment, monitoring, prediction, and prevention of diseases.
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