Development of a Dual-Modal PET/NIR-II Probe of Urofollitropin for Enhanced Follicle-Stimulating Hormone Receptor-Targeted Imaging in Diverse Tumors
文献类型：期刊论文
| 作者 | Sun, Yu2; Qu, Chunrong3; Qian, Kun3; Zhang, Xiao1; Zhao, Jun2; Chen, Hao3; Cheng, Zhen3,4 |
| 刊名 | MOLECULAR PHARMACEUTICS
 |
| 出版日期 | 2025-10-06 |
| 卷号 | 22期号:10页码:6228-6236 |
| 关键词 | urofollitropin FSHR dual-modalprobe PET/CT NIR-II |
| ISSN号 | 1543-8384 |
| DOI | 10.1021/acs.molpharmaceut.5c00961 |
| 英文摘要 | The overexpression of follicle-stimulating hormone receptor (FSHR) in diverse tumors, with low or no expression in normal tissues, makes it a promising target for cancer diagnosis and therapy. Urofollitropin (uFSH), a highly purified form of FSH extracted from the urine of postmenopausal women, is widely used in treating infertility or hypogonadotropic hypogonadism through specifically binding to FSHR expressed on ovaries or granulosa cells in the clinic. Given the specific binding between uFSH and FSHR, the uFSH-derived probe may serve as a potential tool for diagnosing diverse tumors. Therefore, in the present study, using uFSH as the precursor, we developed a dual-modal PET/NIR-II probe named Cu-64-NODAGA-uFSH-CH1055 and studied its binding specificity to FSHR in diverse cancers in vitro and in vivo. In vitro cell assays revealed significantly lower fluorescence in the blocking group than in the unblocking group in U87-MG, HT-29, 143B, and PC-3 tumor cells (p < 0.05). Both in vivo PET/CT and NIR-II imaging demonstrated clear tumor visualization. The U87-MG tumors had the highest radioactive uptake (1.80% +/- 0.23% ID/g), followed by HT-29 (1.25% +/- 0.23% ID/g), 143B (0.98% +/- 0.02% ID/g), and PC-3 (0.75% +/- 0.11% ID/g) (p = 0.024). The same fluorescence signal intensity trend in diverse tumors was found in the NIR-II images, which was consistent with the FSHR expression detected by Western blotting. Both in vitro and in vivo assays showed the specific FSHR-targeting capability of Cu-64-NODAGA-uFSH-CH1055 in diverse tumors, indicating that the uFSH-based dual-modal probe has the potential for the noninvasive visualization of various tumors through PET/CT and NIR-II imaging. |
| WOS关键词 | BREAST-CANCER ; FSH ; EXPRESSION ; SURGERY ; PET ; LH |
| 资助项目 | National Natural Science Foundation of China[82001864] ; National Natural Science Foundation of China[U2267221] ; Shanghai Municipal Science and Technology Major Project[TM202301H003] ; Shandong Laboratory Program[SYS202205] |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001573920800001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/321516]  |
| 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 | Zhao, Jun; Chen, Hao; Cheng, Zhen |
| 作者单位 | 1.Huazhong Univ Sci & Technol, Union Hosp, Tongji Med Coll, Dept Nucl Med, Wuhan 430042, Peoples R China 2.Tongji Univ, Shanghai East Hosp, Dept Nucl Med, Sch Med, Shanghai 200120, 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.Shandong Lab Yantai Drug Discovery, Bohairim Adv Res Inst Drug Discovery, Yantai 264100, Shandong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Yu,Qu, Chunrong,Qian, Kun,et al. Development of a Dual-Modal PET/NIR-II Probe of Urofollitropin for Enhanced Follicle-Stimulating Hormone Receptor-Targeted Imaging in Diverse Tumors[J]. MOLECULAR PHARMACEUTICS,2025,22(10):6228-6236. |
| APA | Sun, Yu.,Qu, Chunrong.,Qian, Kun.,Zhang, Xiao.,Zhao, Jun.,...&Cheng, Zhen.(2025).Development of a Dual-Modal PET/NIR-II Probe of Urofollitropin for Enhanced Follicle-Stimulating Hormone Receptor-Targeted Imaging in Diverse Tumors.MOLECULAR PHARMACEUTICS,22(10),6228-6236. |
| MLA | Sun, Yu,et al."Development of a Dual-Modal PET/NIR-II Probe of Urofollitropin for Enhanced Follicle-Stimulating Hormone Receptor-Targeted Imaging in Diverse Tumors".MOLECULAR PHARMACEUTICS 22.10(2025):6228-6236. |
入库方式： OAI收割
来源：上海药物研究所
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