Tissue plasminogen activator

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Plasminogen activator, tissue
Identifiers
Symbol	PLAT tPA
HUGO	9051
Entrez	5327
OMIM	173370
RefSeq	NM_000930
UniProt	P00750
Other data
EC number	3.4.21.68
Locus	Chr. 8 p12

Tissue plasminogen activator
Systematic (IUPAC) name
Human tissue plasminogen activator
Identifiers
CAS number	105857-23-6
ATC code	B01AD02
PubChem	?
DrugBank	BTD00050
Chemical data
Formula	C2569H3928N746O781S40
Mol. mass	59042.3 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Tissue plasminogen activator (abbreviated PLAT or tPA) is a secreted serine protease which converts the proenzyme plasminogen to plasmin, a fibrinolytic enzyme. Plasminogen is synthesized as a single chain which is cleaved by PLAT into the two chain disulfide linked plasmin. This enzyme plays a role in cell migration and tissue remodeling. Increased enzymatic activity causes hyperfibrinolysis, which manifests as excessive bleeding; decreased activity leads to hypofibrinolysis which can result in thrombosis or embolism.

Contents 1 Gene 2 Applications 3 See also 4 External links

[edit] Gene

Alternative splicing of the PLAT gene, PLAT, produces three transcripts.

[edit] Applications

Recombinant PLAT is used in diseases which feature blood clots, such as myocardial infarction and stroke. To be effective, PLAT must be administered within the first three hours of the event to be given intravenously, or within six hours to be administered through an arterial catheter directly to the site of occlusion. The guideline in Ontario, Canada hospitals for ischemic strokes is that tPA must be given within 3 hours of the onset of symptoms. Because of this, only about 3% of patients qualify for this treatment. Since PLAT dissolves blood clots, there is risk of hemorrhage with its use.

Recently tPA has been used to dissolve a hematoma associated with hemorrhagic strokes and brain injury.

[edit] See also

• Thrombolysis
• Ultrasound-Enhanced Systemic Thrombolysis

[edit] External links

• http://www.americanheart.org/presenter.jhtml?identifier=4751
• http://www.guideline.gov/summary/summary.aspx?doc_id=3422
• Widening the Window : Strategies to buy time in treating ischemic stroke - Scientific American Magazine (August 2005)

v • d • e Antithrombotics (thrombolytics, anticoagulants, and antiplatelet drugs) (B01)
Vitamin K antagonists	Acenocoumarol, Clorindione, Dicumarol (Dicoumarol), Diphenadione, Ethyl biscoumacetate, Phenprocoumon, Phenindione, Tioclomarol, Warfarin
Heparin group (Platelet aggregation inhibitors)	Antithrombin III, Bemiparin, Dalteparin, Danaparoid, Enoxaparin, Heparin, Nadroparin, Parnaparin, Reviparin, Sulodexide, Tinzaparin
Other platelet aggregation inhibitors	Abciximab, Acetylsalicylic acid (Aspirin), Aloxiprin, Beraprost, Ditazole, Carbasalate calcium, Cloricromen, Clopidogrel, Dipyridamole,Eptifibatide, Indobufen, Iloprost, Picotamide, Prasugrel,Prostacyclin, Ticlopidine, Tirofiban, Treprostinil, Triflusal
Enzymes	Alteplase, Ancrod, Anistreplase, Brinase, Drotrecogin alfa, Fibrinolysin, Protein C, Reteplase, Saruplase, Streptokinase, Tenecteplase, Urokinase
Direct thrombin inhibitors	Argatroban, Bivalirudin,Dabigatran, Desirudin, Hirudin, Lepirudin, Melagatran, Ximelagatran
Other antithrombotics	Defibrotide, Dermatan sulfate, Fondaparinux, Rivaroxaban
Non-medicinal	Citrate, EDTA, Oxalate