Design, Synthesis, and Evaluation of 18F-Labeled Tracers Targeting Fibroblast Activation Protein for Brain Imaging

成纤维细胞活化蛋白 体内分布 体内 化学 血脑屏障 胶质瘤 内化 体外 分子成像 中枢神经系统 医学 癌症研究 细胞 生物化学 生物 癌症 内科学 生物技术
作者
Ziyue Yu,Yong Huang,Hualong Chen,Zeng Jiang,Chengze Li,Yi Xie,Zhongjing Li,Xuebo Cheng,Yajing Liu,Shengli Li,Ying Liang,Zehui Wu
出处
期刊:ACS pharmacology & translational science [American Chemical Society]
卷期号:6 (11): 1745-1757 被引量:7
标识
DOI:10.1021/acsptsci.3c00187
摘要

Fibroblast activation protein (FAP) is closely related to central nervous system diseases such as stroke and brain tumors, but PET tracers that can be used for brain imaging have not been reported. Here, we designed, synthesized, and evaluated 18F-labeled UAMC1110 derivatives suitable for brain imaging targeting FAP. By substituting the F atom for the H atom on the aromatic ring of compound UAMC1110, 1a–c were designed and prepared. 1a–c were confirmed to have a high affinity for FAP through molecular docking and enzyme assay. [18F]1a–c were successfully prepared and confirmed to have high affinity. The stability in vivo indicates that no obvious metabolites of [18F]1a,b were found in the plasma 1 h after injection, which is beneficial for brain imaging. In vitro cell uptake experiments showed that [18F]1a,b and [68Ga]FAPI04 exhibited similar uptake and internalization rates. PET imaging of U87MG subcutaneous tumor showed that [18F]1a,b could penetrate the blood–brain barrier with higher uptake and longer retention time than [68Ga]FAPI04 (uptake at 62.5 min, 1.06 ± 0.23, 1.09 ± 0.25% ID/g vs 0.21 ± 0.10% ID/g, respectively). The brain-to-blood ratios of [18F]1a,b were better than [68Ga]FAPI04. Biodistribution and PET imaging showed that [18F]1a had better uptake on tumors and a higher tumor-to-muscle ratio than [18F]1b and [68Ga]FAPI04. Further imaging of U87MG intracranial glioma showed that [18F]1a outlined high-contrast gliomas in a short period of time compared to [18F]1b. Therefore, [18F]1a is expected to be useful in the diagnosis of FAP-related brain diseases.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
1秒前
嗨是完成签到,获得积分10
1秒前
ding应助包子采纳,获得10
1秒前
科目三应助lz采纳,获得10
2秒前
华仔应助不是二次元采纳,获得10
2秒前
xftx发布了新的文献求助10
3秒前
呆萌忆山发布了新的文献求助10
3秒前
所所应助朴实的亿先采纳,获得10
4秒前
西原的橙果完成签到,获得积分10
5秒前
6秒前
DWRH发布了新的文献求助10
7秒前
JamesPei应助moodys采纳,获得10
9秒前
爆米花应助hu采纳,获得10
9秒前
Zxfff发布了新的文献求助10
12秒前
njupt连赛通完成签到,获得积分10
13秒前
勿明应助和谐的万宝路采纳,获得30
13秒前
13秒前
仙贝完成签到,获得积分10
13秒前
缓慢的涵瑶应助DWRH采纳,获得10
14秒前
英俊的铭应助DWRH采纳,获得10
14秒前
吗喽发布了新的文献求助10
16秒前
一一完成签到 ,获得积分10
16秒前
xyzasu完成签到,获得积分10
18秒前
19秒前
希望天下0贩的0应助yoo采纳,获得30
19秒前
melisa发布了新的文献求助10
22秒前
在水一方应助Tin采纳,获得10
22秒前
moodys发布了新的文献求助10
22秒前
云辞忧完成签到,获得积分10
22秒前
复杂的兔子完成签到,获得积分10
23秒前
23秒前
丘比特应助egnaro采纳,获得10
23秒前
24秒前
噗噗完成签到 ,获得积分10
25秒前
完美世界应助白芷采纳,获得10
26秒前
友好的颦完成签到,获得积分20
26秒前
Cyber_relic发布了新的文献求助10
28秒前
赘婿应助初生西红柿采纳,获得10
28秒前
29秒前
深情安青应助科研通管家采纳,获得10
29秒前
高分求助中
【提示信息,请勿应助】关于scihub 10000
The Mother of All Tableaux: Order, Equivalence, and Geometry in the Large-scale Structure of Optimality Theory 3000
Social Research Methods (4th Edition) by Maggie Walter (2019) 2390
A new approach to the extrapolation of accelerated life test data 1000
北师大毕业论文 基于可调谐半导体激光吸收光谱技术泄漏气体检测系统的研究 390
Phylogenetic study of the order Polydesmida (Myriapoda: Diplopoda) 370
Robot-supported joining of reinforcement textiles with one-sided sewing heads 360
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 4010435
求助须知:如何正确求助?哪些是违规求助? 3550258
关于积分的说明 11305330
捐赠科研通 3284688
什么是DOI,文献DOI怎么找? 1810836
邀请新用户注册赠送积分活动 886556
科研通“疑难数据库(出版商)”最低求助积分说明 811470