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Showing 1 to 20 of 61 for “"PAI-1"”.
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Structure-activity relationships of PAI-1 inhibitors
… 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 that …
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Engineering of an anti-PAI-1 antibody with tissue specific activation
… for tissue targeting. By using anti-PAI-1 pro-antibodies to specifically target the kidney for the treatment of chronic kidney disease to minimise observed cardiotoxicities, my work aims to validate this technique as a POC. To this end, I have designed a pro-antibody, based on the …
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Modulation of TGFβ-Induced PAI -1 Expression by Changes in Actin Polymerization in Human Mesangial Cells
… plasminogen actuator inhibitor type-1 (PAI-1; expression. PAI-1 inhibits ECM degradation by tissue- (tPA) and urokinase-type (uPA) plasminogen activators. Additionally, the Rho family of GTPases is required for TGFβ-induced PAI-1 expression. Since, regulation of actin cytoskeletal …
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Auswirkung von Genvariationen im PAI-1- und Leptin-System bei Patienten mit koronarer Herzerkrankung und Restenose nach perkutaner koronarer Intervention
Die Bedeutung von PAI-1 als kardiovaskulärer Risikofaktor ist bekannt. Erhöhte Plasmaspiegel von PAI-1 zeigen in früheren Studien eine Assoziation zum Auftreten kardiovaskulärer Erkrankungen. PAI-1-Gen Polymorphismen könnten Einfluss auf die PAI-1 Expression nehmen und somit ebenfalls mit …
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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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Molecular Insights and Physiological Consequences of Aryl Hydrocarbon Receptor Regulated Plasminogen Activator Inhibitor-1 Expression
… 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 crucial component early in regeneration. …
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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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Thrombophile Genmutationen bei Patientinnen mit rezidivierenden Spontanaborten unklarer Genese
… 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 polymorphism in women with …
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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
… death, we observed ethanol-induced cognitive impairments in adult WT, but not tPA<sup>-/-</sup> mice. To understand how ethanol affects tPA we subjected mice to drugs that mimic the actions of ethanol in the brain. tPA<sup>-/-</sup> mice were protected from neurodegeneration after treatment with …
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The role of platelets and leukocytes in endogenous fibrinolysis.
… blood cells on the plasma activity of t-PA and PAI-1 was measured. In vivo platelet and white blood cell aggregation was induced by platelet and white blood cell agonists, the effect being monitored by the Technicon autocounter. Plasma activity of t-PA and PAI-1 was measured using the amidolytic …
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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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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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Insights Into the Dynamic Structure and Inhibitory Mechanism of Plasminogen Activator Inhibitor Type 1
… the biochemical differences between wild-type PAI-1 (wtPAI-1) and 14-1B and to infer structural and 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 …
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Korrelation von genetischen Polymorphismen mit dem Schweregrad der Intimahyperplasie nach Stentimplantation
… this job investigated the influence of the PAI-1 promoter polymorphism on the "late loss" (a quantitative surrogate of the instent-restenosis) on 300 patients, smokers as well as non-smokers. The 4G/5G promoter polymorphism determines up to 40% of the PAI-1 plasma mirror. Whereas both …
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Design and synthesis of small-molecule inhibitors as anti-malarial and anti-serpin agents
… humans, and plasminogen activator inhibitor-1 (PAI-1), an endogenous serine proteases inhibitor implicated in a wide range of biological processes. Malaria is one of the top global health threats, and there is a great need for developing effective new chemotherapies. PAI-1 is a major component …
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