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Showing 1 to 20 of 20 for “"plasminogen activator inhibitor-1"”.
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Generation of novel small molecules as inhibitors of plasminogen activator inhibitor-1
<p>Plasminogen activator inhibitor (PAI-1) is a member of the serine protease inhibitor (serpin) family of proteins, which inhibits certain serine proteases, such as tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), and thus is a primary regulator of …
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Design, synthesis and evaluation of small molecules as inhibitors of plasminogen activator inhibitor-1
<p>Plasminogen activator inhibitor type-1 (PAI-1) is a member of the serine protease inhibitor (serpin) superfamily. Excessive levels of PAI-1 inhibit urokinase-type plasminogen activator (uPA) and tissue-type plasminogen activator (tPA), which regulates fibrinolysis as well as the development of …
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Molecular Insights and Physiological Consequences of Aryl Hydrocarbon Receptor Regulated Plasminogen Activator Inhibitor-1 Expression
… for suppression of the regenerative response is plasminogen activator inhibitor-1 (PAI-1), which negatively regulates the cleavage and activation of hepatocyte growth factor (HGF) from its latent form in the extracellular matrix. Once activated, HGF signalling through its receptor cMet is a …
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Progress toward a structure-function relationship for novel, small-molecule inhibitors of plasminogen activator inhibitor-1
<p>Plasminogen activator inhibitor-1 (PAI-1) is a serpin protein whose function is to inhibit tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), and hence, fibrinolysis. This inhibition leads to decreased plasminogen to plasmin conversion, which results in …
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Synthesis and structure activity relationship of novel small molecules as inhibitors of plasminogen activator inhibitor-1
<p>Plasminogen activator inhibitor type-1 (PAI-1) is a member of the serine protease inhibitor (serpin) family. PAI-1 is involved in the regulation of fibrinolysis, which is the breakdown of blood clots. PAI-1 inhibits serine proteases tissue-type plasminogen activator (tPA) and urokinase-type …
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Transcriptional Regulation of human Plasminogen Activator Inhibitor-1 Gene Expression by Insulin-like Growth Factor-1, Insulin and Upstream Stimulatory Factor-2
PAI-1 hemmt die Umwandlung des Proenzyms Plasminogen in die aktive Protease Plasmin und moduliert proteolytische Prozesse, die mit prethrombotischen Ereignissen, Thrombose und Hypoxie assoziiert sind. Da Insulin-resistente Stadien durch eine Erhöhung des PAI-1 Spiegels charakterisiert sind haben …
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Design, synthesis, and biological evaluation of non-symmetric smal
<p>Plasminogen activator inhibitor-1 (PAI-1) is a member of the serpin family of proteins, a primary inhibitor of both tissue-type and urokinase-type plasminogen activators in plasma, and is a well-established risk factor in various disease conditions. Increased levels of active PAI-1 in plasma are …
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Structure-activity relationships of PAI-1 inhibitors
<p>The inhibition of plasminogen activator inhibitor-1 (PAI-1) is anticipated to increase our understanding of various human ailments with which high levels of PAI-1 have been associated, including diabetes, stroke, and atherosclerosis. Previous accounts have reported the synthesis of inhibitors …
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Design and synthesis of small-molecule inhibitors as anti-malarial and anti-serpin agents
… synthesis and evaluation of small-molecule inhibitors of two different biological targets: <em>Plasmodium falciparium</em>, the most virulent malarial parasite in humans, and plasminogen activator inhibitor-1 (PAI-1), an endogenous serine proteases inhibitor implicated in a wide range of …
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Differential mechanisms by which the aryl hydrocarbon receptor attenuates liver regeneration
… the c-Met transmembrane receptor and urokinase plasminogen activator (uPA). However, this growth response is limited by the expression of plasminogen activator inhibitor-1 (PAI-1) and TGF-?, which terminates hepatocyte proliferation. The goal of these studies was to determine the influence of …
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Thrombophile Genmutationen bei Patientinnen mit rezidivierenden Spontanaborten unklarer Genese
… spaces. Fibrinolysis is tightly regulated by plasminogen activator inhibitor-1 (PAI-1). Endothelial PAI-1 synthesis is induced by angiotensin II, which is generated by angiotensin I-converting enzyme (ACE). METHODS: We studied the ACE deletion (D)/insertion (I) polymorphism and the PAI-1 4G/5G …
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The ageing hair follicle environment. Alterations in the female scalp and mesenchyme with age.
… Metallopeptidase 1 (MMP1) and Metallopeptidase inhibitor 1 (TIMP1), cyclin-dependent kinase inhibitor 2A (p16INK4A), 11β-Hydroxysteroid dehydrogenase type 1 and 2 (11β-HSD1/HSD11B1 and 11β-HSD2/HSD11B2) mRNA expression increased in aged DFs. In DS cells, HAS2, Vimentin (VIM) ,PDPN, …
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Dietary and Serum Biomarkers, and Glycaemic status: Relationships with Type 2 Diabetes Mellitus and Incident Dementia
… model identified fructosamine, MIC-1, urate, plasminogen activator inhibitor-1, and vitamin E as key dementia predictors. T2D moderated associations between dietary factors and dementia, though no mediation effects were found. Conclusion: Oxidative stress and inflammatory markers like …
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Novel Roles for the Tissue Plasminogen Activator System in the Development of Fetal Alcohol Syndrome and the Regulation of Contextual Learning After Stress
… to as fetal alcohol syndrome (FAS). Since tissue plasminogen activator (tPA) has been implicated in mediating excitotoxic neurodegeneration we subjected neonatal WT and tPA<sup>-/-</sup> to an acute ethanol paradigm that serves as a model of FAS. We observed persistent upregulation of tPA and …
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The Effect of Radiation and Repeated Sub-culturing on TGF-β1 Signaling in FRTL-5 Cells
… expression of its response genes; cyclin A and plasminogen activator inhibitor-1 (PAI-1) under our experimental conditions. To determine this we used luciferase reporter constructs containing promoters for cyclin A and PAI introduced to the cultures by transfection. PAI-1 production in response …
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Bioenergetic and functional impacts of glucose, fructose and insulin in endothelial cells:: implications for cardiovascular disease in diabetes
… tone (NO, endothelin-1) and fibrinolysis (tissue plasminogen activator, plasminogen activator inhibitor-1). These effects were not reversed after acute exposure to NG. Addition of fructose increased markers of metabolic activity, but reduced NO generation. The effect of insulin was complex, …
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Effect of Obesity on the Traditional and Emerging Cardiovascular Disease Risk Factors in African American Women
… high density C-reactive protein [hs-CRP], plasminogen activator inhibitor-1 [PAI-1], E-selectin, quantitative insulin sensitivity check index [QUICKI], and soluble intercellular adhesion molecule-1 [sICAM-1]). Prediabetes and diabetes were determined based on the American Diabetes …
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Global fibrinolytic potential of black South Africans in the North West Province
… three polymorphisms in the promoter area of the plasminogen activator inhibitor-1 (PAI-1) gene on PAI-1act (activity) levels (a main determinant of CLT) and CLT, together with gene-environment interactions and the effect of urbanisation on these interactions. PARTICIPANTS AND METHODS Apparently …
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Mathematical modelling of the innate and adaptive immune response to solid tumours
… the interactions between cancer cells, urokinase plasminogen activator (uPA), plasminogen activator inhibitor-1 (PAI-1), plasmin, extracellular matrix (ECM) and the immune response. The mathematical model focuses on the effect of the immune response on cancer invasion by assuming that there is …