Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.4.21.7 (plasmin)
 9,023 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Five substituted amides of lysine with the general formula: X-Lys-NH-Y, where X= acetyl or ethoxycarbonyl, Y= cyclohexyl, benzyl, hexyl or cadaverine residue were synthesised and their effects on fibrinolytic activity of plasmin, clotting activity of thrombin and amidolytic activities of both enzymes were examined.
Acta Pol Pharm
PMID:Biological activity of amide derivatives of lysine. 1864 58

Inhibitory effects of nine carbocyclic DNA minor groove binders on amidolytic activities of plasmin, trypsin and urokinase were examined. Some of the studied compounds affected plasmin or trypsin activity, but not urokinase activity. One of the pentamidine analogues (5) and two bis-netropsin like compounds (6, 8) were potent inhibitors of plasmin (IC50 equals 90 and 100 microM), whereas an analogue of netropsin (2) was trypsin inhibitor (IC50 = 100 microM).
Acta Pol Pharm
PMID:Effects of netropsin and pentamidine amino analogues on the amidolytic activity of plasmin, trypsin and urokinase. 1866 27

Fibrinolytic system constitutes a part of the haemostasis responsible for the degradation of fibrin deposits. Plasminogen proenzyme, the main component of the fibrinolytic system is activated into its active enzyme form--plasmin by activators, mainly by tissue-type plasminogen activator (t-PA) and urokinase-type plasminogen activator (u-PA). t-PA is the main plasminogen activator in the intravascular fibrinolysis, whereas u-PA is rather involved in the extracellular proteolysis. Fibrinolytic activity can be regulated as well by plasminogen activation inhibition (inhibitors: PAl-1 and PAl-2) as by plasmin activity inhibition (alpha2-antiplasmin). Under physiological conditions a balance between coagulation and fibrinolysis exists, that may be altered under pathophysiological conditions. It has been reported that in the pathogenesis of many diseases, the inflammatory processes, expression of proinflammatory mediators, enhanced tissue factor level and/or impaired fibrinolysis are involved. Inflammation disturbs haemostasis and shifts the haemostatic mechanisms in favor of thrombosis. Moreover, the endothelial dysfunction may contribute to the decrease of antithrombotic properties of vessel wall endothelium. Under pathophysiological conditions where a hypofibrinolytic state occurs, impaired fibrinolysis is considered to be an additional risk factor of thrombosis.
Pol Merkur Lekarski 2009 Oct
PMID:[Dysfunction of fibrinolysis as a risk factor of thrombosis]. 1992 67

The amino analogues of pentamidine with a polymethylene (n = 3 - 6) chain and their chlorambucil derivatives were synthesized. The obtained compounds revealed cytotoxic effect on MCF-7 human breast cancer cell line (IC50 = 22 - 95 +/- 2 pM), mainly by the induction of apoptosis. The topoisomerase I/II inhibition assay and the ethidium displacement assay with the use of pBR322 plasmid DNA were used to the study of mechanism by which the obtained compounds could act. All the compounds are able to bind with DNA and interfere in vitro with the activity of topoisomerase (I and II). The determination of association constants with the use of calf thymus DNA, T4 coliphage DNA, poly(dA-dT)2 and poly(dG-dC)2 showed that the tested compounds bind within minor groove of B-DNA, but not selectively. The alkylating activity of chlorambucil derivatives determined in vitro using a Preussmann test was similar to the activity of chlorambucil. The influence of all the compounds on the amidolytic activity of plasmin and trypsin was also examined. The plasmin activity was inhibited by pentamidine, chlorambucil and aromatic bis-amines (IC50 = 0.1 - 8 mM), whereas the trypsin activity was influenced only by pentamidine.
Acta Pol Pharm
PMID:Amino and chlorambucil analogues of pentamidine--synthesis and biological examinations. 2257 8

Effects of eight short peptides containing lysine and epsilon-aminocaproic acid (EACA) on prolongation of the clot lysis time, as well as hemolytic and antibacterial activities were investigated. Interaction with plasmids pBR322 and pUC19 with the use of ethidium bromide assay and determination of influence on the activity of topoisomerase I and II were also tested. Examined compounds inhibited fibrinolytic activity of plasmin and five of them were more active than EACA. Amides of dipeptides were most active antifibrinolytics (IC50 < 0.2 mM). According to the obtained data, the significant inhibition of fibrinolytic activity of plasmin was not associated with hemolytic effects. Examined compounds did not show antibacterial activity (MIC > 512 mg/L). DNA binding effects determined with the use of ethidium bromide were weak for all peptides and similar to those observed with EACA. Six compounds inhibited topoisomerase II action on supercoiled DNA.
Acta Pol Pharm
PMID:Effect of short peptides containing lysine and epsilon-aminocaproic acid on fibrinolytic activity of plasmin and topoisomerase II action on supercoiled DNA. 2375 33

Mast cells (MCs) are an important component of the immune system. Their physiological function is involved in multiple areas of human physiology, thus symptoms of their increased activation vary greatly from severe allergic reactions, such as anaphylaxis, to chronic symptoms, such as depression or osteoporosis. Studies on mastocytosis revealed a subgroup of patients presenting symptoms of increased MC degranulation, defined as mast cell activation syndrome (MCAS). This population includes patients with primary MCAS with clonal abnormal MCs, who do not fulfill the criteria for mastocytosis. These symptoms often overlap with comorbidities, which makes the diagnosis and treatment of MCAS difficult. The syndrome is diagnosed on the basis of 3 criteria: 1) the presence of typical symptoms; 2) elevation of serum tryptase levels; and 3) response to anti-mediator treatment. The diagnosis of MCAS is important especially in patients with anaphylaxis or osteoporosis who require the use of an epinephrine emergency kit and insect venom immunotherapy. In this review, genetic mechanisms and typical symptoms of MCAS as well as its diagnostic criteria and implications were discussed, with a special emphasis on practical guidance with the aim to improve patient care.
Pol Arch Intern Med 2020 04 30
PMID:How to diagnose mast cell activation syndrome: practical considerations. 3209 78


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