Gallium-68-Labeled ZPDGFRβ Affibody: A Potential PET Probe for Platelet-Derived Growth Factor Receptor β-Expressing Carcinomas

体内分布 正电子发射断层摄影术 多塔 化学 体内 癌症研究 核医学 结合 体外 医学 螯合作用 生物化学 生物 数学分析 生物技术 有机化学 数学
作者
Xin Li,Li Zhao,Mingxing Huang,Rang Wang,Mufeng Li,Hao Yang,Xiaofeng Lu,Huawei Cai,Rong Tian
出处
期刊:Molecular Pharmaceutics [American Chemical Society]
卷期号:20 (2): 1357-1364 被引量:2
标识
DOI:10.1021/acs.molpharmaceut.2c00957
摘要

Platelet-derived growth factor receptor β (PDGFRβ) has been demonstrated to be an effective biomarker for a variety of malignant cancers, and affibody-based PDGFRβ molecules have potential as positron emission tomography (PET) tracers for the diagnosis of cancers. Based on previous pharmacokinetics studies, short-lived positron emission radionuclides, such as fluorine-18 and gallium-68, would be more suitable for affibody-based PET imaging. Thus, in the present study, we prepared a gallium-68-labeled PDGFRβ-targeting dimeric affibody conjugate and evaluated its capability for visualizing malignant tumors by micro-PET/computed tomography (CT) imaging. The PDGFRβ-targeting ZPDGFRβ affibody was conjugated with the p-NCS-Bn-DOTA macrocyclic ligand and radiolabeled with gallium-68 to generate the 68Ga-DOTA-ZPDGFRβ PET probe . Then, several types of malignant carcinoma cells (U-87 MG, LS 174T, A549, H1688, and H446) were used to evaluate the targeted cellular binding capability of the PET probe through in vitro/in vivo cellular assays and whole-body imaging by micro-PET/CT. The 68Ga-DOTA-ZPDGFRβ was successfully prepared with a radiochemical yield of 93% and exhibited ideal stability for up to 4 h at room temperature in vitro. This radioactive conjugate demonstrated specific binding ability with PDGFRβ-expressing U-87 MG cells, which was suppressed by PDGFRβ ligands. The biodistribution of 68Ga-DOTA-ZPDGFRβ indicated fast liver clearance and a kidney-bladder excretion route. The U-87 MG xenografted tumor was clearly visualized with 68Ga-DOTA-ZPDGFRβ at 1 h postinjection using micro-PET/CT imaging. 68Ga-DOTA-ZPDGFRβ is a potential radiopharmaceutical for the diagnosis of PDGFRβ-expressing tumors.
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