Development of an FAP-Targeted PET Probe Based on a Novel Quinolinium Molecular Scaffold
文献类型：期刊论文
| 作者 | Li, Lei6,7,8; Cao, Rui5; Chen, Kaixin6,7,8; Qu, Chunrong6,7; Qian, Kun6,7; Lin, Jia6,7,8; Li, Renda4; Lai, Chaoquan4; Wang, Xiao3; Han, Zijian2 |
| 刊名 | BIOCONJUGATE CHEMISTRY
 |
| 出版日期 | 2024-07-02 |
| 页码 | 9 |
| ISSN号 | 1043-1802 |
| DOI | 10.1021/acs.bioconjchem.4c00214 |
| 通讯作者 | Song, Shaoli(shaoli-song@163.com) ; Zhu, Weiliang(wlzhu@simm.ac.cn) ; Cheng, Zhen(zcheng@simm.ac.cn) |
| 英文摘要 | Fibroblast activation protein (FAP) has recently gained significant attention as a promising tumor biomarker for both diagnosis and therapeutic applications. A series of radiopharmaceuticals based on fibroblast activation protein inhibitors (FAPIs) have been developed and translated into the clinic. Though some of them such as radiolabeled FAPI-04 probes have achieved favorable in vivo imaging performance, further improvement is still highly desired for obtaining radiopharmaceuticals with a high theranostics potential. In this study, we innovatively designed an FAPI ligand SMIC-3002 by changing the core quinoline motif of FAPI-04 to the quinolinium scaffold. The engineered molecule was further radiolabeled with Ga-68 to generate a positron emission tomography (PET) probe, [Ga-68]Ga-SMIC-3002, which was then evaluated in vitro and in vivo. [Ga-68]Ga-SMIC-3002 demonstrated high in vitro stability, nanomolar affinity for FAP (8 nM for protein, 23 nM for U87MG cells), and specific uptake in FAP-expressing tumors, with a tumor/muscle ratio of 19.1 and a tumor uptake of 1.48 +/- 0.03 ID/g% at 0.5 h in U87MG tumor-bearing mice. In summary, the quinolinium scaffold can be successfully used for the development of the FAP-targeted tracer. [Ga-68]Ga-SMIC-3002 not only shows high potential for clinical translation but also offers insights into designing a new generation of FAPI tracers. |
| 资助项目 | National Natural Science Foundation of China[U2267221] ; National Natural Science Foundation of China[81901799] ; Shanghai Municipal Science and Technology Major Project[TM202301H003] ; Gansu Science and Technology Major Project[23ZDFA014] ; Shandong Laboratory Program[SYS202205] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001261362400001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/312128]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Song, Shaoli; Zhu, Weiliang; 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.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China 3.Fudan Univ, Shanghai Canc Ctr, Dept Nucl Med, Shanghai 200032, Peoples R China 4.Northeastern Univ, Coll Life & Hlth Sci, Inst Mol Med, Shenyang 110167, Peoples R China 5.Shanghai Jiao Tong Univ, Shanghai Peoples Hosp 6, Sch Med, Dept Nucl Med, Shanghai 200235, Peoples R China 6.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 7.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, Drug Discovery & Design Ctr,State Key Lab Drug Res, Shanghai 201203, Peoples R China 8.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Lei,Cao, Rui,Chen, Kaixin,et al. Development of an FAP-Targeted PET Probe Based on a Novel Quinolinium Molecular Scaffold[J]. BIOCONJUGATE CHEMISTRY,2024:9. |
| APA | Li, Lei.,Cao, Rui.,Chen, Kaixin.,Qu, Chunrong.,Qian, Kun.,...&Cheng, Zhen.(2024).Development of an FAP-Targeted PET Probe Based on a Novel Quinolinium Molecular Scaffold.BIOCONJUGATE CHEMISTRY,9. |
| MLA | Li, Lei,et al."Development of an FAP-Targeted PET Probe Based on a Novel Quinolinium Molecular Scaffold".BIOCONJUGATE CHEMISTRY (2024):9. |
入库方式： OAI收割
来源：上海药物研究所
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