刺
体内
正电子发射断层摄影术
干扰素基因刺激剂
干扰素
体外
免疫荧光
化学
癌症研究
核医学
医学
物理
生物
生物化学
免疫学
受体
抗体
先天免疫系统
生物技术
热力学
作者
Jianyang Fang,Jingru Zhang,Lingxin Meng,Huifeng Li,Dongsheng Xia,Yaoxuan Wang,Hao Chen,Zhenhuan Liao,Rongqiang Zhuang,Yesen Li,Xianzhong Zhang,Zhide Guo
标识
DOI:10.1021/acs.molpharmaceut.3c01201
摘要
The stimulator of interferon genes (STING) is pivotal in mediating STING-dependent type I interferon production, which is crucial for enhancing tumor rejection. Visualizing STING within the tumor microenvironment is valuable for STING-related treatments, yet the availability of suitable STING imaging probes is limited. In this study, we developed [18F]AlF-ABI, a novel 18F-labeled agent featuring an amidobenzimidazole core structure, for positron emission tomography (PET) imaging of STING in B16F10 and CT26 tumors. [18F]AlF-ABI was synthesized with a decay-corrected radiochemical yield of 38.0 ± 7.9% and radiochemical purity exceeding 97%. The probe exhibited a nanomolar STING binding affinity (KD = 35.6 nM). Upon administration, [18F]AlF-ABI rapidly accumulated at tumor sites, demonstrating significantly higher uptake in B16F10 tumors compared to CT26 tumors, consistent with STING immunofluorescence patterns. Specificity was further validated through in vitro cell experiments and in vivo blocking PET imaging. These findings suggest that [18F]AlF-ABI holds promise as an effective agent for visualizing STING in the tumor microenvironment.
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