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

Vascular occlusion is one of the major causes of mortality and morbidity. Blood vessel blockage can lead to thrombotic complications such as myocardial infarction, stroke, deep venous thrombosis, peripheral occlusive disease, and pulmonary embolism. Thrombolytic therapy currently aims to rectify this through the administration of recombinant tissue plasminogen activator. Research is underway to design an ideal thrombolytic drug with the lowest risk. Despite the potent clot lysis achievable using approved thrombolytic drugs such as alteplase, reteplase, streptokinase, tenecteplase, and some other fibrinolytic agents, there are some drawbacks, such as high production cost, systemic bleeding, intracranial hemorrhage, vessel re-occlusion by platelet-rich and retracted secondary clots, and non-fibrin specificity. In comparison, bacterial staphylokinase, is a new, small-size plasminogen activator, unlike bacterial streptokinase, it hinders the systemic degradation of fibrinogen and reduces the risk of severe hemorrhage. A fibrin-bound plasmin-staphylokinase complex shows high resistance to a2-antiplasmin-related inhibition. Staphylokinase has the potential to be considered as a promising thrombolytic agent with properties of cost-effective production and the least side effects.
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PMID:Bacterial staphylokinase as a promising third-generation drug in the treatment for vascular occlusion. 3167 34

Deep vein thrombosis (DVT) is a major health problem affectinga significant portion of population. Primary complications are Pulmonary Embolism (PE) in the short term and Post-Thrombotic Syndrome (PTS) in the long term. Thrombolytic drugs act by activating plasminogen which in turn forms the enzyme plasmin. Plasmin consequently degrades blood clots by breaking down the fibrin molecules which make up the clots help to degrade the already formed clot. They can be used using different route of administration, doses and durations. The purpose of this systematic review was to assess the outcome of thrombolytic therapy in terms of the efficacy, safety and effectiveness of the medicines. Electronic searches of databases (MEDLINE and Google Scholar) were queried for articles written in English since 2000 GC. A total of 760 results were obtained using the search keys, and after excluding duplicates, 275 articles were selected. Finally, 9 randomized controlled trials (RCTs) which met the language of publication, study design and exclusion criteria were included in this systematic review. The data were obtained from nine trials (6 countries), providing a study-level data of 1309 participants. Almost all studies revealed that thrombolytic treatment was effective in the management of acute DVT. In most of the studies, the rate of rethrombosis was lower in case of thrombolytic than standard management. Hence, addition of thrombolytic results in persistence and increases the clinical benefits. Thrombolytic therapy was very effective in reversing closed veins, in boosting the patency rate,whilereflux was higher in patients treated with anticoagulants. Thrombolytic offers potential advantages over the standard treatment of DVT by reducing the proportion of patients with chronic disabling leg symptoms (such as PTS) by triple in the longer term. However, the incident of major bleeding was higher in patients receiving thrombolytics than anticoagulants.
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PMID:Outcome of Acute Deep Venous Thrombosis Using Standard Treatment versus Thrombolytics: A Literature Review. 3187 95

Thrombosis is a life-threatening pathological condition in which blood clots form in blood vessels, obstructing or interfering with blood flow. Thrombolytic agents (TAs) are enzymes that can catalyze the conversion of plasminogen to plasmin to dissolve blood clots. The plasmin formed by TAs breaks down fibrin clots into soluble fibrin that finally dissolves thrombi. Several TAs have been developed to treat various thromboembolic diseases, such as pulmonary embolisms, acute myocardial infarction, deep vein thrombosis, and extensive coronary emboli. However, systemic TA administration can trigger non-specific activation that can increase the incidence of bleeding. Moreover, protein-based TAs are rapidly inactivated upon injection resulting in the need for large doses. To overcome these limitations, various types of nanocarriers have been introduced that enhance the pharmacokinetic effects by protecting the TA from the biological environment and targeting the release into coagulation. The nanocarriers show increasing half-life, reducing side effects, and improving overall TA efficacy. In this work, the recent advances in various types of TAs and nanocarriers are thoroughly reviewed. Various types of nanocarriers, including lipid-based, polymer-based, and metal-based nanoparticles are described, for the targeted delivery of TAs. This work also provides insights into issues related to the future of TA development and successful clinical translation.
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PMID:Thrombolytic Agents: Nanocarriers in Controlled Release. 3279


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