Development of a Novel 18F-Labeled Probe for PET Imaging of Estrogen Receptor beta
文献类型：期刊论文
| 作者 | Zhou, Yujing1,2,4; Lei, Peng1; Han, Jiaxin5; Wang, Zhiming1; Ji, Aiyan1; Wu, Yuyang1; Zheng, Lingling1,3,4; Zhang, Xiaoqing1,4; Qu, Chunrong1; Min, Jian7,8 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2023-01-05 |
| 页码 | 11 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.2c00761 |
| 通讯作者 | Xu, Zhijian(zjxu@simm.ac.cn) ; Liu, Xingdang(xingdliu@fudan.edu.cn) ; Chen, Hao(haoc@simm.ac.cn) ; Cheng, Zhen(zcheng@simm.ac.cn) |
| 英文摘要 | Estrogen receptor beta (ER beta) is an important ER subtype that plays crucial roles in many physiological and pathological disorders. Herein, we developed the probe [18F]PVBO for in vivo ER beta targeted PET imaging and obtained promising results. The nonradioactive PVBO showed a 12.5-fold stronger binding affinity to ER beta than to ER alpha in vitro. In vitro assays revealed the specific uptake of [18F]PVBO by DU145 cells. The uptake of [18F]PVBO by DU145 xenografts increased during the 120 min dynamic scanning, with a maximum uptake of 2.80 +/- 0.30% ID/g. Based on time activity curves (TACs), the injection of [18F]PVBO with unlabeled PVBO or ERB041 resulted in a significant signal reduction with the tumor/muscle (T/M) ratio <1 at 30, 60, 75, and 120 min post-injection (p < 0.05). [18F]PVBO demonstrates the feasibility of noninvasively imaging ER beta-positive tumors by small-animal PET and provides a new strategy for visualizing ER beta in vivo. |
| WOS关键词 | ER-BETA ; SELECTIVE RADIOLIGAND ; BREAST ; ALPHA ; RNA ; EXPRESSION ; PROSTATE ; LIGANDS ; DESIGN |
| 资助项目 | National Key Research and Development Program of China[2021YFC2100300] ; STI2030-Major Projects[2021ZD0203900] ; Lingang Laboratory[LG-QS-202206-01] ; National Natural Science Foundation of China[82071976] ; National Natural Science Foundation of China[81901799] ; National Natural Science Foundation of China[U2267221] ; Shanghai Pujiang Program[19PJ1411100] ; Shanghai Municipal Science and Technology Major Project ; National Key Research and Development Plan Digital Diagnosis and Treatment Equipment Research and Development Project[2017YFC0113300] ; Pudong Hospital, Fudan University, college project[YJYJRC202108] ; Pudong Hospital, Fudan University, college project[YJYJRC202101] ; Pudong Hospital, Fudan University, college project[Zdzk2020-14] ; Shandong Provincial Natural Science Foundation[ZR2022QH315] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:000911960500001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/303817]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Xu, Zhijian; Liu, Xingdang; Chen, Hao; Cheng, Zhen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Shandong Lab Yantai Drug Discovery, Bohai Rim Adv Res Inst Drug Discovery, Yantai 264117, Peoples R China 3.Fudan Univ, Huashan Hosp, Dept Nucl Med, Shanghai 200040, Peoples R China 4.Fudan Univ, Pudong Hosp, Dept Nucl Med, Shanghai 201399, Peoples R China 5.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China 6.Shandong Univ, Qilu Hosp, Dept Nucl Med, Jinan 250012, Shandong, Peoples R China 7.Hubei Collaborat Innovat Ctr Green Transformat Bio, State Key Lab Biocatalysis & Enzyme Engn, Wuhan 430062, Hubei, Peoples R China 8.Hubei Univ, Sch Life Sci, Key Lab Ind Biotechnol, Wuhan 430062, Hubei, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Yujing,Lei, Peng,Han, Jiaxin,et al. Development of a Novel 18F-Labeled Probe for PET Imaging of Estrogen Receptor beta[J]. JOURNAL OF MEDICINAL CHEMISTRY,2023:11. |
| APA | Zhou, Yujing.,Lei, Peng.,Han, Jiaxin.,Wang, Zhiming.,Ji, Aiyan.,...&Cheng, Zhen.(2023).Development of a Novel 18F-Labeled Probe for PET Imaging of Estrogen Receptor beta.JOURNAL OF MEDICINAL CHEMISTRY,11. |
| MLA | Zhou, Yujing,et al."Development of a Novel 18F-Labeled Probe for PET Imaging of Estrogen Receptor beta".JOURNAL OF MEDICINAL CHEMISTRY (2023):11. |
入库方式： OAI收割
来源：上海药物研究所
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