前列腺癌是全球男性第二高发的恶性肿瘤，因此前列腺癌的诊断十分重要。当前临床上使用最多的分子影像手段PSMA PET/CT成像会因PSMA蛋白水平下降，导致不能检出前列腺癌。一些研究表明，促红细胞生成素产生肝细胞受体相互作用蛋白A型受体2(erythropoietin-producing hepatomocellular receptor-interacting protein type-A receptor 2, EphA2)为PSMA PET/CT不能检出的前列腺癌提供了可能靶点。

因此本课题设计并合成了靶向EphA2的荧光探针ETF与核素探针前体ETN。在细胞水平上论证了靶向EphA2的荧光探针ETF对PSMA阴性前列腺癌细胞系的显像能力。PET/CT显像与生物分布实验验证了¹⁸F标记的核素探针[¹⁸F]AlF-ETN可在PSMA-的PC3肿瘤模型中特异性富集，注射1h后肿瘤摄取值最高达2.67%ID/g。靶向EphA2的探针对前列腺癌的检测可以弥补当前PSMA PET/CT检测的局限性，对前列腺癌的诊疗具有重要的意义。

The diagnosis of prostate cancer is important as it is the second most prevalent malignancy in men worldwide. PSMA PET/CT imaging, currently the most used molecular imaging tool in clinical practice, can fail to detect prostate cancer due to decreased PSMA levels. Several studies have shown that erythropoietin-producing hepatomocellular receptor-interacting protein type-A receptor 2 (EphA2) provides a possible target for prostate cancers that cannot be detected by PSMA PET/CT.

Therefore, a fluorescent probe ETF and a nuclear probe precursor ETN targeting EphA2 have been designed and synthesised in this project. The ability of ETF, a fluorescent probe targeting EphA2, to visualise PSMA negative prostate cancer cell lines was demonstrated at the cellular level. PET/CT imaging and biodistribution experiments demonstrated that the ¹⁸F-labelled probe [¹⁸F]AlF-ETN was specifically enriched in the PSMA- PC3 tumour model with a maximum tumour uptake value of 2.67% ID/g 1h after injection. The detection of prostate cancer with probes targeting EphA2 can compensate for the limitations of current PSMA PET/CT detection and is important for the diagnosis and treatment of prostate cancer.