Urokinase
| Urokinase | ||
|---|---|---|
|
Existing structural data: see UniProt entry |
||
| Properties of human protein | ||
| Mass / length primary structure | 411 amino acids | |
| Secondary to quaternary structure | Heterodimer A + B | |
| Identifier | ||
| Gene name | PLAU | |
| External IDs |
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| Drug information | ||
| ATC code | B01 AD04 | |
| DrugBank | DB00013 | |
| Drug class | Fibrinolytic | |
| Enzyme classification | ||
| EC, category | 3.4.21.73 , serine protease | |
| MEROPS | S01.231 | |
| Substrate | Arg - + - Val in plasminogen | |
| Products | Plasmin | |
| Occurrence | ||
| Homology family | Trypsin | |
| Parent taxon | Creature | |
Urokinase or urokinase-type plasminogen activator ( uPA for short ) is an enzyme from the group of peptidases (also proteases ) that is used to treat myocardial infarction , pulmonary embolism and other thrombotic vascular occlusions as well as for the therapy and prophylaxis of thrombotic catheter occlusions.
Urokinase was first discovered in human urine and described as a protease . Physiologically, it circulates in the bloodstream and converts plasminogen into plasmin , which is a serine proteinase that dissolves various proteins in the plasma and in particular fibrin clots. This process is known as fibrinolysis and the effectiveness of urokinase as a drug is based on this mechanism. Urokinase is inhibited by the plasminogen activator inhibitors PAI-1 and PAI-2.
It was found that the expression of urokinase and PAI-1 is significantly increased in various cancer diseases and can thus serve as a prognostic marker.
Its effect can be reversed by administering tranexamic acid .
Urokinase receptor
When urokinase is bound to its cellular receptor , the urokinase receptor (uPAR) attached to the cell membrane by a glycosylphosphatidylinositol anchor (GPI anchor) , its proteolytic activity is greatly increased. In addition, the binding of urokinase to the uPAR activates mitotic signaling pathways of the cell and increases cellular migration. These processes are independent of the proteolytic activity of urokinase.
Indications
Urokinase is approved in Germany for use at
- Peripheral arterial thrombosis
- acute and subacute deep vein thrombosis
- acute, diagnostically confirmed pulmonary embolism, especially in unstable hemodynamic conditions
- thrombosed arteriovenous shunt
- for the prophylaxis of infectious and thrombotic complications of central venous catheters
- Restoration of the patency of thrombotic occluded central venous catheters, including hemodialysis catheters.
Trade names
Urokinase is approved in Germany, Austria and Switzerland under the name Urokinase HS medac in five strengths (10,000 / 50,000 / 100,000 / 250,000 / 500,000 IU), but has not been available for some time.
Individual evidence
- ↑ Medac: https://s3.eu-central-1.amazonaws.com/prod-cerebro-ifap/media_all/47017.pdf (PDF; 66 kB)
- ↑ Urokinase delivery failure. Retrieved January 28, 2020 (German).
