新型前列腺癌靶向药物68Ga-NOTA-GC-PSMA用于前列腺癌成像的临床前评估

IF 2.2 4区医学 Q2 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING

Tomography Pub Date : 2025-03-07 DOI:10.3390/tomography11030029

Wenjin Li, Yihui Luo, Yuqi Hua, Qiaoling Shen, Liping Chen, Yu Xu, Haitian Fu, Chunjing Yu

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引用次数: 0

摘要

目的：前列腺特异性膜抗原（PSMA）靶向放射配体是前列腺癌（PCa）靶向正电子发射断层扫描（PET）成像的有前途的诊断工具。在目前的工作中，我们旨在开发一种新的PSMA示踪剂，为前列腺癌诊断提供额外的选择。方法：我们团队设计了一种新的PSMA示踪剂结构，并通过体外细胞实验对其进行了评价，初步验证了68Ga-NOTA-GC-PSMA的靶向性和特异性。PET/CT对psma阳性异种移植模型进行体内显像，进一步验证放射性示踪剂的体内特异性和靶向性。将前列腺癌患者病理组织切片与病理免疫组化及放射自显影实验病理组织染色结果进行比较，评估68Ga-NOTA-GC-PSMA对人前列腺癌病理组织的靶向作用。结果：新型示踪剂亲水性高，清除率快。特异性细胞结合和微pet成像实验表明，68Ga-NOTA-GC-PSMA具有高特异性LNCaP肿瘤细胞摄取（120 min时为1.70%±0.13%）和肿瘤与肌肉（T/M）、肿瘤与肾脏（T/K）比（60 min时分别为13.87±11.20和0.20±0.08）。结论：新型示踪剂68Ga-NOTA-GC-PSMA是一种有前景的前列腺癌放射性核素显像。

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Preclinical Evaluation of a Novel PSMA-Targeted Agent ⁶⁸Ga-NOTA-GC-PSMA for Prostate Cancer Imaging.

Objectives: Prostate-specific membrane antigen (PSMA)-targeted radioligands are promising diagnostic tools for the targeted positron emission tomography (PET) imaging of prostate cancer (PCa). In present work, we aimed to develop a novel PSMA tracer to provide an additional option for prostate cancer diagnosis. Methods: Our team designed a new structure of the PSMA tracer and evaluated it with cellular experiments in vitro to preliminarily verify the targeting and specificity of ⁶⁸Ga-NOTA-GC-PSMA. PET/CT imaging of PSMA-positive xenograft-bearing models in vivo to further validate the in vivo specificity and targeting of the radiotracer. Pathological tissue sections from prostate cancer patients were compared with pathological immunohistochemistry and pathological tissue staining results by radioautography experiments to assess the targeting-PSMA of ⁶⁸Ga-NOTA-GC-PSMA on human prostate cancer pathological tissues. Results: The novel tracer showed high hydrophilicity and rapid clearance rate. Specific cell binding and micro-PET imaging experiments showed that ⁶⁸Ga-NOTA-GC-PSMA displayed a high specific LNCaP tumor cell uptake (1.70% ± 0.13% at 120 min) and tumor-to-muscle (T/M) and tumor-to-kidney (T/K) ratio (13.87 ± 11.20 and 0.20 ± 0.08 at 60 min, respectively). Conclusions: The novel tracer ⁶⁸Ga-NOTA-GC-PSMA is promising radionuclide imaging of PCa.

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来源期刊

Tomography Medicine-Radiology, Nuclear Medicine and Imaging

CiteScore

2.70

自引率

10.50%

发文量

222

期刊介绍： TomographyTM publishes basic (technical and pre-clinical) and clinical scientific articles which involve the advancement of imaging technologies. Tomography encompasses studies that use single or multiple imaging modalities including for example CT, US, PET, SPECT, MR and hyperpolarization technologies, as well as optical modalities (i.e. bioluminescence, photoacoustic, endomicroscopy, fiber optic imaging and optical computed tomography) in basic sciences, engineering, preclinical and clinical medicine. Tomography also welcomes studies involving exploration and refinement of contrast mechanisms and image-derived metrics within and across modalities toward the development of novel imaging probes for image-based feedback and intervention. The use of imaging in biology and medicine provides unparalleled opportunities to noninvasively interrogate tissues to obtain real-time dynamic and quantitative information required for diagnosis and response to interventions and to follow evolving pathological conditions. As multi-modal studies and the complexities of imaging technologies themselves are ever increasing to provide advanced information to scientists and clinicians. Tomography provides a unique publication venue allowing investigators the opportunity to more precisely communicate integrated findings related to the diverse and heterogeneous features associated with underlying anatomical, physiological, functional, metabolic and molecular genetic activities of normal and diseased tissue. Thus Tomography publishes peer-reviewed articles which involve the broad use of imaging of any tissue and disease type including both preclinical and clinical investigations. In addition, hardware/software along with chemical and molecular probe advances are welcome as they are deemed to significantly contribute towards the long-term goal of improving the overall impact of imaging on scientific and clinical discovery.