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Tissue plasminogen activator

From Wikipedia, the free encyclopedia

Crystal structure of the protease domain of tPA in complex with an inhibitor
Plasminogen activator, tissue
Identifiers
Symbol(s) PLAT tPA
Entrez 5327
OMIM 173370
RefSeq NM_000930
UniProt P00750
Other data
EC number 3.4.21.68
Locus Chr. 8 p12
Image:Tissue plasminogen activator.png
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. weight 59042.3 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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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

[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 six or so hours of the attack. 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.

[edit] See also

[edit] External links


 v  d  e 
Coagulation
Coagulation factors: - Fibrin (I) - (Pro)thrombin (II) - FV - FVII - FVIII - FIX - FX - FXI - FXII - FXIII - HMWK - vWF - Tissue factor
Inhibitors: Antithrombin - Protein C - Protein S - Protein Z - ZPI - TFPI
Fibrinolysis: Plasmin - tPA/urokinase - PAI-1/2 - α2-AP - TAFI
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