Development of a novel 18F-labeled small molecule probe for PET imaging of mesenchymal epithelial transition receptor expression
文献类型：期刊论文
| 作者 | Bu, Lihong6,7,8; Ma, Xiaowei5; Ji, Aiyan3,4; Geng, Kaijun2; Feng, Hongyan8; Li, Li8; Zhang, Ao2; Cheng, Zhen1,4,6,7 |
| 刊名 | EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
 |
| 出版日期 | 2023-11-09 |
| 页码 | 13 |
| 关键词 | Mesenchymal epithelial transition receptor Gliomas [18F]-AZC PET Quinoline derivative compound |
| ISSN号 | 1619-7070 |
| DOI | 10.1007/s00259-023-06495-8 |
| 通讯作者 | Zhang, Ao(ao6919zhang@sjtu.edu.cn) ; Cheng, Zhen(zcheng@simm.ac.cn) |
| 英文摘要 | The mesenchymal epithelial transition factor (c-Met) is frequently overexpressed in numerous cancers and has served as a validated anticancer target. Inter- and intra-tumor heterogeneity of c-Met, however, challenges the use of anti-MET therapies, highlighting an urgent need to develop an alternative tool for visualizing whole-body c-Met expression quantitatively and noninvasively. Here we firstly reported an F-18 labeled, small-molecule quinine compound-based PET probe, 1-(4-(5-amino-7-(trifluoromethyl) quinolin-3-yl) piperazin-1-yl)-2-(fluoro-[18F]) propan-1-one, herein referred as [18F]-AZC.Methods [18F]-AZC was synthesized via a one-step substitution reaction and characterized by radiochemistry methods. [18F]-AZC specificity and affinity toward c-Met were assessed by cell uptake assay, with or without cold compound [19F]-AZC or commercial c-Met inhibitor blocking. MicroPET/CT imaging and biodistribution studies were conducted in subcutaneous murine xenografts of glioma. Additionally, [18F]-AZC was then further evaluated in orthotopic glioma xenografts, by microPET/CT imaging accompanied with MRI and autoradiography for co-registration of the tumor. Immunofluorescence staining was also carried out to qualitatively evaluate the c-Met expression in tumor tissue, co-localizes with H&E staining.Results This probe shows easy radiosynthesis, high stability in vitro and in vivo, high targeting affinity, and favorable lipophilicity and brain transport coefficient. [18F]-AZC demonstrates excellent tumor imaging properties in vivo and can delineate c-Met positive glioma specifically at 1 h after intravenous injection of the probe. Moreover, favorable correlation was observed between the [18F]-AZC accumulation and the amount of c-Met expression in tumor.Conclusion This novel imaging probe could be applied as a valuable tool for management of anti-c-Met therapies in patients in the future. |
| WOS关键词 | FACTOR/HEPATOCYTE GROWTH-FACTOR ; TIVANTINIB ARQ 197 ; C-MET EXPRESSION ; ANTITUMOR-ACTIVITY ; KINASE INHIBITORS ; IN-VITRO ; GLIOBLASTOMA ; CELLS |
| 资助项目 | This work was supported in part by the International Collaboration Key Program of Chinese Academy of Sciences (GJHZ1622), the National Basic Research Program of China 973 program (2015CB91063), the Office of Science (BER), US Department of Energy (DE-SC0[GJHZ1622] ; International Collaboration Key Program of Chinese Academy of Sciences[2015CB91063] ; National Basic Research Program of China 973 program[DE-SC0008397] ; Office of Science (BER), US Department of Energy[P50 CA114747] ; NIH In vivo Cellular Molecular Imaging Center ; Chinese Academy of Sciences[U2267221] ; Chinese Academy of Sciences[81871419] ; Chinese Academy of Sciences[81430080] ; Chinese Academy of Sciences[81125021] ; Chinese Academy of Sciences[81501501] ; National Science Foundation of China[TM202301H003] ; Shanghai Municipal Science and Technology Major Project |
| WOS研究方向 | Radiology, Nuclear Medicine & Medical Imaging |
| 语种 | 英语 |
| WOS记录号 | WOS:001101955500002 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/307848]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhang, Ao; 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, Shanghai Frontiers Sci Ctr Drug Target Identificat, Sch Pharmaceut Sci, Natl Key Lab Innovat Immunotherapy, Shanghai 200240, Peoples R China 3.Fudan Univ, Sch Pharm, Dept Pharm, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, Shanghai Inst Mat Med,Chinese Acad Sci, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China 5.Cent South Univ, PET CT Ctr, Xiangya Hosp 2, Changsha 410011, Hunan, Peoples R China 6.Stanford Univ, Biox Program, Stanford, CA 94305 USA 7.Stanford Univ, Dept Radiol, Mol Imaging Program Stanford MIPS, Stanford, CA 94305 USA 8.Wuhan Univ, Renmin Hosp, PET CT MRI Ctr, Wuhan 430060, Peoples R China |
| 推荐引用方式 GB/T 7714 | Bu, Lihong,Ma, Xiaowei,Ji, Aiyan,et al. Development of a novel 18F-labeled small molecule probe for PET imaging of mesenchymal epithelial transition receptor expression[J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,2023:13. |
| APA | Bu, Lihong.,Ma, Xiaowei.,Ji, Aiyan.,Geng, Kaijun.,Feng, Hongyan.,...&Cheng, Zhen.(2023).Development of a novel 18F-labeled small molecule probe for PET imaging of mesenchymal epithelial transition receptor expression.EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,13. |
| MLA | Bu, Lihong,et al."Development of a novel 18F-labeled small molecule probe for PET imaging of mesenchymal epithelial transition receptor expression".EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2023):13. |
入库方式： OAI收割
来源：上海药物研究所
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