Molecular Imaging Center, University of Southern California, Los Angeles, CA 90033, USA.
Theranostics. 2013 Jun 29;3(7):507-15. doi: 10.7150/thno.5557. Print 2013.
Urokinase-type plasminogen activator receptor (uPAR) is a glycosylphosphatidylinositol (GPI)-anchored protein. Besides regulating proteolysis, uPAR could also activate many intracellular signaling pathways that promote cell motility, invasion, proliferation, and survival through cooperating with transmembrane receptors. uPAR is overexpressed across a variety of tumors and is associated with cancer invasion and metastasis. In order to meet the demand for a rapid development and potential clinical application of anti-cancer therapy based on uPA/uPAR system, it is desirable to develop non-invasive imaging methods to visualize and quantify uPAR expression in vivo. In this review, we will discuss recent advances in the development of uPAR-targeted nuclear imaging and radionuclide therapy agents. The successful development of molecular imaging probes to visualize uPAR expression in vivo would not only assist preclinical researches on uPAR function, but also eventually impact patient management.
尿激酶型纤溶酶原激活物受体（uPAR）是一种糖基磷脂酰肌醇（GPI）锚定蛋白。除了调节蛋白水解作用外，uPAR 还可以通过与跨膜受体合作激活许多促进细胞运动、侵袭、增殖和存活的细胞内信号通路。uPAR 在多种肿瘤中过度表达，并与癌症侵袭和转移有关。为了满足基于 uPA/uPAR 系统的癌症治疗快速发展和潜在临床应用的需求，人们希望开发非侵入性成像方法来在体内可视化和定量 uPAR 的表达。在这篇综述中，我们将讨论开发针对 uPAR 的核成像和放射性核素治疗剂的最新进展。成功开发用于体内可视化 uPAR 表达的分子成像探针不仅将有助于 uPAR 功能的临床前研究，而且最终还将影响患者管理。
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