Neha Patil (Editor)

Plasminogen activator

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Aliases
  
PLG, Plasmin

Human
  
Mouse

Ensembl
  
ENSG00000122194

Species
  
Human

Entrez
  
5340

Plasminogen activator

External IDs
  
MGI: 97620 HomoloGene: 55452 GeneCards: PLG

Tissue plasminogen activator tpa


Plasminogen activators are serine proteases that catalyze the activation of plasmin via proteolytic cleavage of its zymogen form plasminogen. Plasmin is an important factor in fibrinolysis, the breakdown of fibrin polymers formed during blood clotting. There are two main plasminogen activators: urokinase (uPA) and tissue plasminogen activator (tPA). Tissue plasminogen activators are used to treat medical conditions related to blood clotting including embolic or thrombotic stroke, myocardial infarction, and pulmonary embolism.

Contents

Plasminogen activators are inhibited by plasminogen activator inhibitor-1, plasminogen activator inhibitor-2, and protein C inhibitor.

tpa tissue plasminogen activator 5 minute door to needle youtube


Function

Produced mainly in the liver, plasminogen is the inactive zymogen form of plasmin, and circulates in plasma in a closed conformation that cannot be activated. Binding clots or cell surface causes its conformation to change, allowing it to be activated by plasminogen activators. Plasminogen activators do so by cleaving the R561/V562 peptide bond, producing the active protein plasmin, which catalyzes the degradation of fibrin polymers that make up the structure of blood clots.

Applications

Due to its contribution to fibrinolysis, tissue plasminogen activator is used medically to treat blood clot-related disorders including thrombotic or embolic stroke, myocardial infarction, and pulmonary embolism. It is manufactured using recombinant techniques and is sold as alteplase, reteplase, and tenecteplase. Alteplase was the first of these versions to go on the market, and has the same exact structure as tPA. Reteplase and tenecteplase both received FDA approval after alteplase, and have nonidentical structures to tPA.

Urokinase is similarly used in the medical field, specifically for the treatment of pulmonary embolism.

References

Plasminogen activator Wikipedia