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Showing 1 to 20 of 32 for “"Plasminogen Activator Inhibitor"”.
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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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In vivo and in vitro regulation of plasminogen activator inhibitor type-1
… switch from producing a mixture of active tissue plasminogen activator (t-PA) and urokinase (u-PA) to producing active u-PA alone. I performed a series of experiments designed to examine the mechanism of down regulation of t-PA activity that occurred with differentiation. The results of these …
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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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Insights Into the Dynamic Structure and Inhibitory Mechanism of Plasminogen Activator Inhibitor Type 1
… functional details about the naturally occurring inhibitor using the structural model of the stable variant as a starting point. Using conformationally-sensitive ligands, we found that the RCL of PAI-1 exhibited more partial insertion into the beta-sheet A and that beta-sheet A was more accessible …
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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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Der Einfluss von HMG-COA-Reduktase-Inhibitoren auf die Genexpression in kultivierten humanen Endothelzellen
… der Statine erklärt werden könnten sowie der plasminogen activator inhibitor (PAI1), der im Rahmen der Blutgerinnung seinen Einfluss entfaltet. <br>Insgesamt lässt sich sagen, dass insbesondere die Verkettung der Lipidsenker mit der Expression des hsp47 und des BNP die bis dato bekannten Daten …
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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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Mapping Major Genetic Factors of Obesity
… leptin, resistin, tumor necrosis factor alpha, plasminogen activator inhibitor one, interleukin six, insulin, and oxytocin) involved in pathways that affect metabolism. Behaviors like hyperphagia and exercise are important aspects of both the development and treatment of the disease. All 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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Proteolytic mechanisms involved in the metastasis of human melanoma cells
… which could contribute to the process, plasminogen activation by tissue plasminogen activator (tPA) and urokinase plasminogen activator (uPA) is one such mechanism. Extensive reports in the literature (reviewed in the introduction) indicate that most tumour cells synthesize uPA and that …
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