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近年来随着分子生物技术的飞速发展,医学研究者对肿瘤侵袭和转移的分子机制有了进一步了解,其中尿激酶型纤溶酶原激活物(urokinase plasminogen activator,uPA)及其特异性受体(urokinase plasminogen activator receptor,uPAR)的表达备受关注[1-3]。uPA/uPAR是基质降解酶系统的重要组成之一,肿瘤细胞分泌的uPA是纤溶酶形成的启动物,uPA与uPAR结合后被激活,通过蛋白水解及信号传导途径启动一系列反应,对肿瘤的侵袭和转移有明显的促进作用,还可通过上调凋亡抑制因子的表达,起到抑制肿瘤细胞凋亡的作用[4-9]。uPA/uPAR在多种肿瘤组织中高表达,其表达不仅是肿瘤侵袭与转移的核心环节,还与肿瘤的恶性程度与不良预后密切相关。以uPAR为靶向的治疗已成为肿瘤治疗新途径[10-13],放射性核素靶向显像可提供肿瘤uPAR表达水平高低的信息。近年来,很多课题组对uPAR靶向显像进行了研究并发表了他们的研究成果,综述如下。
uPAR放射性核素靶向显像研究进展
Research progress of uPAR-targeted nuclear imaging
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摘要: 尿激酶型纤溶酶原激活物及其特异性受体(uPA/uPAR)系统是肿瘤侵袭、转移和血管生成的核心环节之一, 且与肿瘤的不良预后密切相关。检测肿瘤组织中uPA/uPAR表达水平及其随病情的变化情况, 对于肿瘤预后判断、治疗方案的选择与疗效评价意义重大。放射性核素分子靶向显像方法在靶向受体表达水平测定上具有独特的优势, 近来年医学研究者使用多种放射性核素标记uPAR的特异性配体进行了动物显像研究, 并于2015年首次用于人体显像。笔者就近年来uPAR放射性核素靶向显像的研究进展作一综述。Abstract: Urokinase plasminogen activator(uPA) and urokinase plasminogen activator receptor(uPAR) system play an important role in the process of cancer invasion, metastasis and angiogenesiss, and it is closely associated with poor prognosis of tumors. Evaluate of uPAR expression level in the tumor cell is very significant for cancer prognosis, selection and assement the therapy. Molecular targeted nuclear imaging has unique advantage in testing receptor expression, several research group labeled uPAR specially ligands with different radionuclides for imaging uPAR. The first human uPAR imaging has taken in 2015. This article reviewed the research progress of uPAR-targeted molecular nuclear imaging in recent years.
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Key words:
- Radionuclide imaging /
- Urinary plasminogen activator /
- Targeted imaging
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