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agriculture
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effect of urokinase-type plasminogen activator on in vitro embryo production. Urokinase-type plasminogen activator added to the 18 h in vitro maturation medium significantly increases embryo development rates
analysis
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assay of cellular internalization and localization of enzyme:PAI-2 inhibitor complex based on the use of inhibitor labelled with Alexa488 fluorochrome and a polyclonal antibody
analysis
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optical zymography technique that specifically detects enzyme activity in biological samples via fluorescence emission at 695 nm. Method can efficiently distinguish the active two-chain enzyme from its proenzyme and directly measure enzyme activities in different cancer cell lines
analysis
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quantification of uPA and inhibitor PAI-1 mRNA expression in breast cancer cell lines as well as in tumor tissue of breast cancer patients by sensitive quantitative real-time PCR assays, based on the LightCycler technology. In breast cancer cell lines, mRNA and antigen values are highly correlated for both uPA and PAI-1 I. Correlations between uPA/PAI-1 mRNA and protein in the breast cancer samples were found to be distinctly weaker or not significant. Quantitative determination of mRNA expression for both factors does not mirror antigen levels in breast cancer tissue
diagnostics
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expression level of uPA in prostate cancer tissue can be used as a predictor of biochemical recurrence in patients undergoing radical prostatectomy, i.e. strong expression of uPA in addition to a Gleason score, positive surgical margin, and lymph node metastasis
diagnostics
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uPA is the strongest single indicator of poor prognosis in patients with metastatic breast cancer
diagnostics
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urokinase-type plasminogen activator is a marker of aggressive phenotype and an independent prognostic factor in mismatch repair-proficient colorectal cancer, overview
drug development
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the enzyme is an attractive target for the development of small molecule active site inhibitors
drug development
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uPA is a potential therapeutic target in a variety of pathological conditions, including cancer
drug development
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complex formation of uPA and uPAR is a target for development of therapeutics
medicine
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associated with tumor metastasis and invasion, selective inhibitors of uPA may have potential as therapeutically useful drugs for prostate, breast and other cancers
medicine
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active enzyme promotes tumor progression, activation of enzyme appears as a key step in tumor progression. Inhibition of enzyme with natural or synthetic inhibitors diminishes high intravasating Matrigel invasion in vitro and intravasation and metastasis in vivo
medicine
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after infection with staphylococci, level of metabolically active enzyme is unaltered in plasma but significantly decreased in kidney homogenate. Enzyme acts as endogenous antibacterial substance. Decrease in enzyme level in infected organs may be due to dramatically increased production of plasminogen activator inhibitor type I
medicine
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amino-terminal fragment ATF of urokinase exerts an antitumor effect via dual mechanisms: essentially through targeting the uPA-uPAR system via the EGF-like domain and partially through targeting a uPAR-indepedent interaction via the kringle domain
medicine
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amino-terminal fragment ATF of urokinase exerts an antitumor effect via dual mechanisms: essentially through targeting the uPA-uPAR system via the EGF-like domain and partially through targeting a uPAR-indepedent interaction via the kringle domain
medicine
treatment of cancer with small-molecule active-site inhibitors with a C-terminal 4-amindinobenzylamide residue to prevent metastasis. Inhibitor dose of 2 x 1.5 mg/kg/day of inhibitor N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide reduces number of metastases to 4.6% in mice
medicine
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all patients examined with common variable immunodeficiency had increased plasma levels of soluble uPA receptor with particularly high levels in those with splenomegaly and thrombocytopenia. Plasma uPA levels were also raised in these patients, and both soluble uPA receptor and uPA levels correlated with the monocyte activation marker neopterin. Monocytes from patients with common variable immunodeficiency had increased expression of uPA receptor
medicine
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brain tissue of thermally injured rats displays an increase in the brain water content and the presence of Evans blue, temporally associated with an increased expression of endogenous tPA and uPA. Peripheral thermal injury does induce an increase in the permeability of the blood brain barrier
medicine
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either uPA/uPAR interaction, Mac-1 activation, or prevention of its association with uPAR triggers a signaling pathway leading to the inefficient release of HIV from monocytic cells
medicine
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expression of uPA, its receptor, and of inhibitor PAI-1 is increased in response to Helicobacter pylori, and for uPA, but not the receptor or PAI-1, requires the virulence factor CagE. Helicobacter pylori also stimulates soluble and cell surface-bound uPA activity. It stimulates epithelial cell proliferation, which is inhibited by uPA immunoneutralization and uPA receptor knock-down. Expogenous uPA also stimulates proliferation that is further increased after PAI-1 knock-down
medicine
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in a severe combined immunodeficient-human mouse model, PC-3 cells are the major source of uPA in the experimental bone tumor. Injection of uPA-silenced PC-3 cells in bone xenografts results in significant reduction of bone tumor burdens and protection of trabecular bones from destruction. The suppressed tumor growth is associated with the level of uPA expression but not with its activity. An increase in the expression of PAI-1, the endogenous uPA inhibitor, is found during in vitro tumor-stromal interactions. Up-regulation of PAI-1 in bone stromal cells and preosteoclasts/osteoblasts is due to soluble factor(s) released by PC cells, and the enhanced PAI-1 expression in turn stimulated PC cell migration
medicine
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in cancer cell, expression of uPA and uPA receptor underlies a mechanism of stem cell tropism to malignant tumors
medicine
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in mice model for kidney ischemia reperfusion injury, deficiency for uPA receptor, but not uPA protects from ischemia reperfusion injury. In the allogenic kidney transplant model, uPA receptor but not uPA deficiency of the allograft causes superior recipient survival and strongly attenuates loss of renal function. uPA receptor-deficient allografts show reduced generation of reactive oxygen species and apoptosis. Neutrophil and monocyte/macrophage infiltration is strongly attenuated and up-regulation of the adhesion molecule ICAM-1 is completely abrogated in uPA receptor-deficient allografts
medicine
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in patients with colorectal cancer, the protease antigen levels are significantly higher compared with other groups. At the time of clinical detection proteases cathepsin B, cathepsin L and urokinase-type plasminogen activator and its inhibitor are more sensitive indicators for colorectal cancer than commonly used tumor markers. Determination of cathepsin B, cathepsin L and urokinase-type plasminogen activator and its inhibitor have a major prognostic impact in patients with colorectal cancer
medicine
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in sputum derived from patients with house dust mite allergic asthma, the medium concentration of uPA is significantly greater than in healthy control patients. The sputum concentration of uPA correlates with sputum total cell count and with logarithmically transformed exhaled nitric oxide concentration, but not with FEV1 or bronchial reactivity to histamine. Tge effect of uPA seems to be independent of its fibrinolytic activity
medicine
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induction of lateral fluid percussion brain injury results in up-regulation of uPA and ERK mitogen-activated protein kinase. uPA contributes to the impairment of sodium nitroprusside and PGE2-mediated cerebrovasodilatation through activation of low-density lipoprotein receptor and ERK mitogen-activated protein kinase
medicine
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possible involvement of uPA in natural killer cell-mediated immune surveillance and tumor escape. Addition of uPA to natural killer cell receptor Ly49E positive adult and fetal natural killer cells inhibits interferon-gamma secretion and reduces their cytotoxic potential, respectively
medicine
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quantification of uPA and inhibitor PAI-1 mRNA expression in breast cancer cell lines as well as in tumor tissue of breast cancer patients by sensitive quantitative real-time PCR assays, based on the LightCycler technology. In breast cancer cell lines, mRNA and antigen values are highly correlated for both uPA and PAI-1 I. Correlations between uPA/PAI-1 mRNA and protein in the breast cancer samples were found to be distinctly weaker or not significant. Quantitative determination of mRNA expression for both factors does not mirror antigen levels in breast cancer tissue
medicine
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silencing of transmembrane protein Notch1 expression by siRNa inhibits invasion of human prostate cancer cells by inhibiting the expression of matrix metalloproteinase-9 and uPA
medicine
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study on cocaine-induced conditioned-place preference in rats with bilateral intra-accumbens injections of uPA-expressing lentiviral vectors. Overexpression of uPA in the nucleus accumbens significantly augments cocaine-induced place preference. Reinstatement with a low dose of cocaine produces significantly greater preference to the cocaine-associated context. Once cocaine-induced conditioned-place preference has been established, and the preference extinguished, reinstatement induced by a priming dose of cocaine is facilitated by uPA. Inhibition of tuPA expression abolishes the augmented acquisition produced by overexpression of uPA but not the expression of the cocaine-induced conditioned-place preference. When uPA is inhibited during the acquisition phase, animals no longer demonstrate place preference for the environment previously paired with cocaine. B428, a specific uPA inhibitor does not affect drug reinstatement after extinction if uPA has been activated during acquisition. Cocaine-induced conditioned-place preference and reinstatement may be dependent on active extracellular uPA
medicine
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the levels of uPA and uPA receptor in patients with acute or chronic hepatitis B significantly exceeds those in healthy controls. Patients with severe chronic hepatitis B have significantly higher levels of uPA and uPA receptor than those with moderate and mild chronic disease and those with acute hepatitis B. The plasma uPA and uPA receptor levels markedly increase in the acute stage and dramatically decrease in the remission stage, but in all stages levels exceede those in healthy subjects. The concentration of plasma uPA receptor is positively correlated with prothrombin and total bilirubin
medicine
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the overexpression of uPA in Quebec platelet disease emerges with megakaryocyte differentiation, without altering the expression of flanking genes. uPA is costored with-granule proteins prior to their proteolysis in Quebec platelet disease
medicine
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uPA promotes inward arterial remodeling by regulating oxidative stress and inflammation after arterial injury
medicine
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uPA, seprase and pipeptidylaminopeptidase IV immunoreactivity is found in dysplastic and cancer cells as well as in stromal cells adjacent to dysplasia and cancer sites, but not in normal epithelium. There is a significant association between uPA expression and sex, tumor size and histological classification in carcinomas. Squamous cell carcinoma lines display higher levels of uPA, seprase and dipeptidylaminopeptidase IV than normal esophageal epithelial cell lines
medicine
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macrophages, recruited into venous thrombi, can be used to target uPA gene constructs to the thrombus after systemic administration
medicine
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co-operation between TIMP-1 and host uPA suggests that therapies, simultaneously interfering with pro- and anti-proteolytic pathways may be beneficial for patients with metastatic disease
medicine
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co-operation between TIMP-1 and host uPA suggests that therapies, simultaneously interfering with pro- and anti-proteolytic pathways may be beneficial for patients with metastatic disease
medicine
inhibition of the enzyme might be beneficial in treating cancer
pharmacology
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rapid, sensitive and selective method for detection of uPA activator UK-356202 in human plasma using column-switching HPLC and fluorescence detection. The limit of detection is 20 pg/ml, and the method is linear over a 100-fold concentration range
pharmacology
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Treatment of nude mice bearing subcutaneously or orthotopically implanted human colon cancer cell lines HCT-116 and HT-29 with TX-1877, irradiation or TX-1877 with irradiation results in significant inhibition of matrix metalloproteinase-9 and uPA. Treatments also inhibit the para-aortic lymph node metastasis, however, do not prolong the survival in orthotopic model. In the subcutaneous model, tumors treated with TX-1877 and irradiation show significant reductions in volume
pharmacology
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uPA blocking antibodies may not be indicated for cancer growth inhibition strategies, but may serve as valuable tools for the implementation of pharmacodelivery strategies against a variety of different tumors