Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer
文献类型：期刊论文
| 作者 | Luo, Xiangning4,5; Luo, Renli4; Zhou, Yuanyuan4; Jiang, Yuanpeng4; Han, Cong4; Song, Aiguo1,3,4; Qian, Kun4; Qu, Chunrong4; Cao, Rui2; Xu, Bin5 |
| 刊名 | NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
 |
| 出版日期 | 2025-07-01 |
| 卷号 | 67页码:9 |
| 关键词 | Gastrin-releasing peptide receptor 68Ga Dar chelator Positron emission tomography Imaging probe |
| ISSN号 | 1549-9634 |
| DOI | 10.1016/j.nano.2025.102829 |
| 英文摘要 | 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. |
| WOS关键词 | CONJUGATED BOMBESIN ANTAGONIST ; PEPTIDE RECEPTOR-ANTAGONIST ; LU-177-AMBA |
| 资助项目 | National Natural Science Foundation of China[U2267221] ; State Key Laboratory of Drug Research[SIMM0120231004] ; Gansu Science and Technology Major Project[23ZDFA014] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDB0830300] ; Shandong Laboratory Program[SYS202205] |
| WOS研究方向 | Science & Technology - Other Topics ; Research & Experimental Medicine |
| 语种 | 英语 |
| WOS记录号 | WOS:001501575700001 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/318258]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Cao, Rui; Xu, Bin; Cheng, Zhen |
| 作者单位 | 1.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China 2.Shanghai Jiao Tong Univ, Sch Med, Dept Nucl Med, Shanghai Peoples Hosp 6, Shanghai 200235, Peoples R China 3.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China 5.Shanghai Univ, Innovat Drug Res Ctr, Dept Chem, Shanghai 200444, Peoples R China |
| 推荐引用方式 GB/T 7714 | Luo, Xiangning,Luo, Renli,Zhou, Yuanyuan,et al. Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer[J]. NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,2025,67:9. |
| APA | Luo, Xiangning.,Luo, Renli.,Zhou, Yuanyuan.,Jiang, Yuanpeng.,Han, Cong.,...&Cheng, Zhen.(2025).Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer.NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,67,9. |
| MLA | Luo, Xiangning,et al."Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer".NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE 67(2025):9. |
入库方式： OAI收割
来源：上海药物研究所
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