中文摘要：

胞外蛋白的水解是恶性肿瘤细胞侵袭和转移的必要条件，各种蛋白酶的水解反应降解细胞外基质，破坏细胞／细胞间的联系以适应细胞的迁移。尿激酶型纤溶酶原激活物（尿激酶，urokinase—typeplasminogen activator，uPA）激活不具有丝氨酸蛋白酶活性的纤溶酶原为活性纤溶酶，在保持血流畅通与防止血栓的形成中具有重要的作用。此外，活性尿激酶降解细胞外基质，激活多种基质金属蛋白酶，以适应肿瘤细胞的侵袭、扩散和转移。抑制尿激酶的活性被公认为是抑制癌症转移的有效方法，其中合成小分子uPA抑制剂成为抗癌治疗中的新理念。本文综述了合成uPA抑制剂的研究现状。

英文摘要：

The extracellular proteolysis is the necessary condition for the malignant process of tumor invasion and metastasis. These proteolytic reactions destruct the cell-cell and cell/ECM contacts and degrade the extracellular matrix （ECM） components which pose physical obstacle in the direction of migration/invasion. Urokinase-type plasminogen activator （uPA）, which can activate the inactive plasminogen to plasmin, plays a pivotal role in clot lysis and keeps the blood flowing. Moreover, active uPA degrades ECM and activates a number of matrix metalloproteases, beginning a cascade of events adapting to the cancer cell invasion, spread and metastasis. The inhibition of uPA activity has been recognized as an efficient method in the treatment of cancer by retarding tumor growth and metastasis and inhibition of urokinase with synthetic inhibitor is a new concept for specific cancer therapy. Here we review the current research status of synthetic uPA inhibitors.