Invited reviewThe urokinase plasminogen activator system as a novel target for tumour therapy
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Cited by (128)
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA)
2012, Bioorganic and Medicinal ChemistryCitation Excerpt :An amidine based, peptide-derived inhibitor (1, Fig. 1) reduces the number of experimental lung metastases in a fibrosarcoma model in mice,12 and two clinical phase I trials with uPA inhibitors 2a (WX-UK1)13 and its prodrug 2b (WX-671 or MESUPRON®) have been successfully completed. Moreover, compound 2b showed favorable results in randomized phase II trial in patients with locally advanced nonmetastatic pancreatic cancer and phase II trial in patients with HER2-negative metastatic breast cancer (MBC) has been initiated.14 Wendt et al. reported a series of substituted naphthamidines as inhibitors of uPA (3a–c as representative examples) and 3c was shown to possess high selectivity towards tPA, thrombin and plasmin.15
Dependence on endocytic receptor binding via a minimal binding motif underlies the differential prognostic profiles of serpinE1 and serpinB2 in cancer
2011, Journal of Biological ChemistryCitation Excerpt :very low density lipoprotein receptor Combined tumor overexpression of uPA, its receptor (uPAR), and SerpinE1 (serine protease inhibitor E1) is strongly correlated with poor patient prognosis (1–3) and metastatic potential (4–8). Consequently, uPA and SerpinE1 expression is recommended as an independent prognostic indicator in node-negative breast cancer (9).
Expression of urokinase plasminogen activator and its receptor in advanced epithelial ovarian cancer patients
2009, Gynecologic OncologyCitation Excerpt :uPA is strongly implicated as a promoter of tumor progression in various human malignancies, and is synthesized and secreted as a pro-enzyme. uPA is activated by binding with high affinity specific membrane-bound or soluble cell surface uPA receptors (uPAR), which efficiently convert plasminogen, into plasmin, that directly or indirectly cleaves ECM components [5]. Plasmin can also activate latent elastase and matrix metalloproteinases (MMPs), which can also degrade ECM components [6].
Co-Expression of Urokinase With Haptoglobin in Human Carcinomas
2009, Journal of Surgical ResearchProtease Inhibitors of Marine Origin: Promising Anticancer and HIV Therapies
2023, Biomedical Research, Medicine, and Disease