A Novel Radiotracer for NTSR1-Targeted PET Imaging of Tumor: Preclinical and First-in-Human Studies
文献类型：期刊论文
| 作者 | Zhu, Jiamin1,3; Yuan, Hui2; Tan, Boyu3,6,7; Liu, Xiufeng2; Qian, Kun3; Jiang, Yuanpeng1,3; Li, Renda3,5; Zhang, Wenqing1,3; Qu, Chunrong3; Cheng, Zhen1,3,4 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2025-12-11 |
| 卷号 | 68期号:23页码:25186-25197 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.5c02195 |
| 英文摘要 | Neurotensin receptor 1 (NTSR1) is overexpressed in various cancers, making it an attractive target for tumor imaging and therapy. However, current NTSR1-targeting peptides derived from neurotensin (NT) analogs face challenges including rapid metabolic clearance and insufficient tumor uptake, limiting their clinical translation. To address this, we developed a novel probe, [Ga-68]Ga-DOTA-NT-20.3-IPBA, by conjugating the DOTA-NT-20.3 probe with an albumin-binding moiety (4-(p-iodophenyl)butyric acid [IPBA]). The resulting tracer exhibited enhanced lipophilicity and albumin-binding capacity, while maintaining reasonable in vitro stability, radiochemical yield, and purity (all >95%). In vitro and in vivo evaluations confirmed its high affinity and specificity for NTSR1. Clinical PET/CT imaging demonstrated significant tracer accumulation in lung adenocarcinoma, with a tumor-to-lung ratio of 7.89 +/- 0.76 at 60 min postinjection and a favorable biodistribution profile. Collectively, [Ga-68]Ga-DOTA-NT-20.3-IPBA shows high potential as a PET tracer for NTSR1-expressing tumors and DOTA-NT-20.3-IPBA may be a promising candidate for future theranostic development. |
| WOS关键词 | NEUROTENSIN ; RECEPTOR ; CANCER ; EXPRESSION ; THERAPY ; PEPTIDE ; GROWTH |
| 资助项目 | Chinese Academy of Sciences[XDB0830300] ; Ningbo Major Research and Development Plan Project[2024Z214] ; Natural Science Foundation of Shanghai Municipality[24ZR1477300] ; Gansu Science and Technology Major Project[23ZDFA014] ; National Natural Science Foundation of China[81971645] ; Shandong Laboratory Program[SYS202205] ; Guangdong Provincial People?s Hospital[KY0120211130] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001626514900001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/322076]  |
| 专题 | 国家级研究中心_原创新药研究全国重点实验室 |
| 通讯作者 | Qu, Chunrong; Cheng, Zhen; Jiang, Lei |
| 作者单位 | 1.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China 2.Southern Med Univ, Guangdong Prov Peoples Hosp, Guangdong Acad Med Sci, PET Ctr,Dept Nucl Med, Guangzhou 510080, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Bohai Rim Adv Res, Yantai 264117, Shandong, Peoples R China 5.Northeastern Univ, Inst Mol Med, Coll Life & Hlth Sci, Shenyang 110819, Peoples R China 6.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 7.ShanghaiTech Univ, Sch Biomed Engn, Shanghai 201210, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Jiamin,Yuan, Hui,Tan, Boyu,et al. A Novel Radiotracer for NTSR1-Targeted PET Imaging of Tumor: Preclinical and First-in-Human Studies[J]. JOURNAL OF MEDICINAL CHEMISTRY,2025,68(23):25186-25197. |
| APA | Zhu, Jiamin.,Yuan, Hui.,Tan, Boyu.,Liu, Xiufeng.,Qian, Kun.,...&Jiang, Lei.(2025).A Novel Radiotracer for NTSR1-Targeted PET Imaging of Tumor: Preclinical and First-in-Human Studies.JOURNAL OF MEDICINAL CHEMISTRY,68(23),25186-25197. |
| MLA | Zhu, Jiamin,et al."A Novel Radiotracer for NTSR1-Targeted PET Imaging of Tumor: Preclinical and First-in-Human Studies".JOURNAL OF MEDICINAL CHEMISTRY 68.23(2025):25186-25197. |
入库方式： OAI收割
来源：上海药物研究所
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