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
{"title":"基于Dar衍生物的前列腺癌grpr靶向PET探针的设计与合成","authors":"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","doi":"10.1016/j.nano.2025.102829","DOIUrl":null,"url":null,"abstract":"<div><div>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, [<sup>68</sup>Ga]Ga-Dar-C5-P2-RM26 and [<sup>68</sup>Ga]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, [<sup>68</sup>Ga]Ga-Dar-C5-P2-RM26 and [<sup>68</sup>Ga]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, [<sup>68</sup>Ga]Ga-Dar-C5-RM26 and [<sup>68</sup>Ga]Ga-Dar-RM26 are GRPR-targeted radiotracers with high potential for clinical translation in tumor-targeted imaging.</div></div>","PeriodicalId":19050,"journal":{"name":"Nanomedicine : nanotechnology, biology, and medicine","volume":"67 ","pages":"Article 102829"},"PeriodicalIF":4.6000,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design and synthesis of GRPR-targeted PET probes based on Dar derivatives for imaging of prostate cancer\",\"authors\":\"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\",\"doi\":\"10.1016/j.nano.2025.102829\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>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, [<sup>68</sup>Ga]Ga-Dar-C5-P2-RM26 and [<sup>68</sup>Ga]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, [<sup>68</sup>Ga]Ga-Dar-C5-P2-RM26 and [<sup>68</sup>Ga]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, [<sup>68</sup>Ga]Ga-Dar-C5-RM26 and [<sup>68</sup>Ga]Ga-Dar-RM26 are GRPR-targeted radiotracers with high potential for clinical translation in tumor-targeted imaging.</div></div>\",\"PeriodicalId\":19050,\"journal\":{\"name\":\"Nanomedicine : nanotechnology, biology, and medicine\",\"volume\":\"67 \",\"pages\":\"Article 102829\"},\"PeriodicalIF\":4.6000,\"publicationDate\":\"2025-05-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Nanomedicine : nanotechnology, biology, and medicine\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1549963425000292\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"MEDICINE, RESEARCH & EXPERIMENTAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nanomedicine : nanotechnology, biology, and medicine","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1549963425000292","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"MEDICINE, RESEARCH & EXPERIMENTAL","Score":null,"Total":0}
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.
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.