Identification

Name
Tenecteplase
Accession Number
DB00031  (BTD00019, BIOD00019)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Thrombolytic agents
Description

Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.

Protein structure
Db00031
Protein chemical formula
C2561H3919N747O781S40
Protein average weight
58951.2 Da
Sequences
>DB00031 sequence
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGG
TCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGNWSTAESGAECTNWQSSA
LAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDC
YFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAK
PWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAAAAAS
PGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVH
KEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEAL
SPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGG
PLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
Download FASTA Format
Synonyms
  • TNK-tPA
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MetalyseInjection, powder, for solution10000 unitsIntravenousBoehringer Ingelheim2001-02-23Not applicableEu
MetalyseInjection, powder, for solution8000 unitsIntravenousBoehringer Ingelheim2001-02-23Not applicableEu
TNKaseKitGenentech, Inc.2000-06-02Not applicableUs
TnkasePowder, for solution50 mgIntravenousHoffmann La Roche2001-10-18Not applicableCanada
Categories
UNII
WGD229O42W
CAS number
191588-94-0

Pharmacology

Indication

For treatment of myocardial infarction and lysis of intracoronary emboli

Structured Indications
Pharmacodynamics

Tenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.

Mechanism of action

Tenecteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.

TargetActionsOrganism
APlasminogen
activator
Human
AFibrinogen alpha chainNot AvailableHuman
UUrokinase plasminogen activator surface receptorNot AvailableHuman
UPlasminogen activator inhibitor 1Not AvailableHuman
UPlasminogen activator inhibitor 2Not AvailableHuman
UTetranectinNot AvailableHuman
UKeratin, type II cytoskeletal 8Not AvailableHuman
UAnnexin A2Not AvailableHuman
UCalreticulinNot AvailableHuman
UCalnexinNot AvailableHuman
UProlow-density lipoprotein receptor-related protein 1Not AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)

Clearance
  • 99 - 119 mL/min [acute myocardial infarction patients]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Tenecteplase Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabTenecteplase may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolTenecteplase may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Tenecteplase.Approved, Vet Approved
AloxiprinThe risk or severity of adverse effects can be increased when Aloxiprin is combined with Tenecteplase.Experimental
AlprostadilAlprostadil may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Tenecteplase.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Tenecteplase.Approved
AncrodTenecteplase may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Tenecteplase.Investigational
Antithrombin III humanTenecteplase may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanTenecteplase may increase the anticoagulant activities of Apixaban.Approved
AprotininThe therapeutic efficacy of Tenecteplase can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinTenecteplase may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanTenecteplase may increase the anticoagulant activities of Argatroban.Approved, Investigational
AzelastineAzelastine may increase the anticoagulant activities of Tenecteplase.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Tenecteplase.Approved, Investigational
BecaplerminTenecteplase may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BeraprostBeraprost may increase the anticoagulant activities of Tenecteplase.Investigational
BivalirudinTenecteplase may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BuflomedilBuflomedil may increase the anticoagulant activities of Tenecteplase.Experimental
ButylphthalideButylphthalide may increase the anticoagulant activities of Tenecteplase.Investigational
CangrelorCangrelor may increase the anticoagulant activities of Tenecteplase.Approved
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Tenecteplase.Experimental
CertoparinTenecteplase may increase the anticoagulant activities of Certoparin.Approved
CilostazolCilostazol may increase the anticoagulant activities of Tenecteplase.Approved
Citric AcidTenecteplase may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Tenecteplase.Approved, Nutraceutical
CloricromenCloricromen may increase the anticoagulant activities of Tenecteplase.Experimental
Dabigatran etexilateTenecteplase may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinTenecteplase may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidTenecteplase may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanTenecteplase may increase the anticoagulant activities of Darexaban.Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Tenecteplase.Investigational
DesirudinTenecteplase may increase the anticoagulant activities of Desirudin.Approved
DextranTenecteplase may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Tenecteplase may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Tenecteplase may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Tenecteplase may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolTenecteplase may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Tenecteplase.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Tenecteplase.Approved
Edetic AcidTenecteplase may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanTenecteplase may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinTenecteplase may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
EplivanserinEplivanserin may increase the anticoagulant activities of Tenecteplase.Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Tenecteplase.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Tenecteplase.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
Ethyl biscoumacetateTenecteplase may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ferulic acidTenecteplase may increase the anticoagulant activities of Ferulic acid.Experimental
FluindioneTenecteplase may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxTenecteplase may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumTenecteplase may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateTenecteplase may increase the anticoagulant activities of Gabexate.Investigational
GuacetisalThe risk or severity of adverse effects can be increased when Guacetisal is combined with Tenecteplase.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Tenecteplase.Experimental
HeparinTenecteplase may increase the anticoagulant activities of Heparin.Approved, Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Tenecteplase.Investigational
IbudilastIbudilast may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Tenecteplase.Approved, Nutraceutical
IdraparinuxTenecteplase may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Tenecteplase.Approved, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Tenecteplase.Investigational
IloprostIloprost may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
IndobufenIndobufen may increase the anticoagulant activities of Tenecteplase.Investigational
KetanserinKetanserin may increase the anticoagulant activities of Tenecteplase.Investigational
LepirudinTenecteplase may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanTenecteplase may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Tenecteplase.Approved
LinsidomineLinsidomine may increase the anticoagulant activities of Tenecteplase.Experimental
MelagatranTenecteplase may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Tenecteplase.Approved
MilrinoneMilrinone may increase the anticoagulant activities of Tenecteplase.Approved
NadroparinTenecteplase may increase the anticoagulant activities of Nadroparin.Approved
NafamostatTenecteplase may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Tenecteplase.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Tenecteplase.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Tenecteplase.Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Tenecteplase.Approved
OtamixabanTenecteplase may increase the anticoagulant activities of Otamixaban.Investigational
Pentosan PolysulfateTenecteplase may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
PhenindioneTenecteplase may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonTenecteplase may increase the anticoagulant activities of Phenprocoumon.Approved
PicotamidePicotamide may increase the anticoagulant activities of Tenecteplase.Experimental
PrasugrelPrasugrel may increase the anticoagulant activities of Tenecteplase.Approved
Protein CTenecteplase may increase the anticoagulant activities of Protein C.Approved
Protein S humanTenecteplase may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeTenecteplase may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Tenecteplase.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Tenecteplase.Experimental, Investigational
ReviparinTenecteplase may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Tenecteplase.Approved
RivaroxabanTenecteplase may increase the anticoagulant activities of Rivaroxaban.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Tenecteplase.Approved, Vet Approved
SarpogrelateSarpogrelate may increase the anticoagulant activities of Tenecteplase.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Tenecteplase.Approved, Vet Approved
SRT501SRT501 may increase the anticoagulant activities of Tenecteplase.Investigational
SulodexideTenecteplase may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TesmilifeneTesmilifene may increase the anticoagulant activities of Tenecteplase.Investigational
TiclopidineTiclopidine may increase the anticoagulant activities of Tenecteplase.Approved
TirofibanTirofiban may increase the anticoagulant activities of Tenecteplase.Approved
TranilastTranilast may increase the anticoagulant activities of Tenecteplase.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Tenecteplase.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Tenecteplase is combined with Treprostinil.Approved, Investigational
TriflusalTriflusal may increase the anticoagulant activities of Tenecteplase.Approved
TroxerutinTenecteplase may increase the anticoagulant activities of Troxerutin.Investigational
VorapaxarVorapaxar may increase the anticoagulant activities of Tenecteplase.Approved
WarfarinTenecteplase may increase the anticoagulant activities of Warfarin.Approved
XimelagatranTenecteplase may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

General References
  1. Gurbel PA, Hayes K, Bliden KP, Yoho J, Tantry US: The platelet-related effects of tenecteplase versus alteplase versus reteplase. Blood Coagul Fibrinolysis. 2005 Jan;16(1):1-7. [PubMed:15650539]
  2. Melzer C, Richter C, Rogalla P, Borges AC, Theres H, Baumann G, Laule M: Tenecteplase for the treatment of massive and submassive pulmonary embolism. J Thromb Thrombolysis. 2004 Aug;18(1):47-50. [PubMed:15744554]
  3. Ohman EM, Van de Werf F, Antman EM, Califf RM, de Lemos JA, Gibson CM, Oliverio RL, Harrelson L, McCabe C, DiBattiste P, Braunwald E: Tenecteplase and tirofiban in ST-segment elevation acute myocardial infarction: results of a randomized trial. Am Heart J. 2005 Jul;150(1):79-88. [PubMed:16084152]
  4. De Luca G, Suryapranata H, Chiariello M: Tenecteplase followed by immediate angioplasty is more effective than tenecteplase alone for people with STEMI. Commentary. Evid Based Cardiovasc Med. 2005 Dec;9(4):284-7. Epub 2005 Nov 2. [PubMed:16380055]
  5. Authors unspecified: Primary versus tenecteplase-facilitated percutaneous coronary intervention in patients with ST-segment elevation acute myocardial infarction (ASSENT-4 PCI): randomised trial. Lancet. 2006 Feb 18;367(9510):569-78. [PubMed:16488800]
External Links
UniProt
P00750
Genbank
L00153
KEGG Drug
D06070
ChEMBL
CHEMBL2108791
Therapeutic Targets Database
DAP000204
PharmGKB
PA164776757
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Tenecteplase
ATC Codes
B01AD11 — Tenecteplase
AHFS Codes
  • 20:12.20 — Thrombolytic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1WithdrawnTreatmentAcute Respiratory Distress Syndrome (ARDS)1
1, 2Unknown StatusTreatmentAcute Myelogenous Leukaemia (AML) / Myelodysplastic Syndrome1
2CompletedTreatmentAcute Myocardial Infarction (AMI)1
2CompletedTreatmentStroke, Ischemic1
2Not Yet RecruitingTreatmentCerebral Artery / Nervous System Disorders1
2RecruitingTreatmentCerebral Infarctions / Ischemia, Brain / Strokes1
2RecruitingTreatmentStroke, Ischemic1
2TerminatedTreatmentLeukemias1
2TerminatedTreatmentStrokes1
2TerminatedTreatmentProphylaxis of Pulmonary embolism1
2Unknown StatusTreatmentStrokes1
2, 3CompletedTreatmentMyocardial Infarction (MI)1
2, 3TerminatedTreatmentPleural Effusions1
2, 3WithdrawnTreatmentStroke, Ischemic1
3Active Not RecruitingTreatmentProphylaxis of Pulmonary embolism1
3CompletedTreatmentDysfunctional Central Venous Access Catheters2
3CompletedTreatmentDysfunctional Hemodialysis Catheters2
3CompletedTreatmentMyocardial Infarction (MI)3
3CompletedTreatmentStroke, Ischemic1
3Not Yet RecruitingTreatmentStroke, Acute / Stroke, Ischemic1
3Not Yet RecruitingTreatmentStroke, Ischemic1
3RecruitingTreatmentPleural Empyema1
3RecruitingTreatmentStroke, Acute1
3TerminatedTreatmentHeart Arrest1
3TerminatedTreatmentProphylaxis of Pulmonary embolism1
3Unknown StatusTreatmentMyocardial Infarction (MI)1
4RecruitingTreatmentAcute Coronary Syndromes (ACS)1
4RecruitingTreatmentMyocardial Infarction (MI)1
4RecruitingTreatmentST Elevation Myocardial Infarction (STEMI)1
4TerminatedTreatmentAcute Myocardial Infarction (AMI)1
4TerminatedTreatmentMyocardial Infarction (MI)1
Not AvailableCompletedNot AvailableMyocardial Infarction (MI)3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionIntravenous10000 units
Injection, powder, for solutionIntravenous8000 units
Kit
Powder, for solutionIntravenous50 mg
Prices
Unit descriptionCostUnit
Tnkase 50 mg kit3238.76USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2129660No2005-06-282013-05-28Canada
CA1341432No2003-06-172020-06-17Canada

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)60 °CNovokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)
hydrophobicity-0.528Not Available
isoelectric point7.61Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Activator
General Function
Serine-type peptidase activity
Specific Function
Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In...
Gene Name
PLG
Uniprot ID
P00747
Uniprot Name
Plasminogen
Molecular Weight
90568.415 Da
References
  1. Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235]
  2. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
General Function
Structural molecule activity
Specific Function
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function ...
Gene Name
FGA
Uniprot ID
P02671
Uniprot Name
Fibrinogen alpha chain
Molecular Weight
94972.455 Da
References
  1. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656]
  2. Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Urokinase plasminogen activator receptor activity
Specific Function
Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-...
Gene Name
PLAUR
Uniprot ID
Q03405
Uniprot Name
Urokinase plasminogen activator surface receptor
Molecular Weight
36977.62 Da
References
  1. Maupas-Schwalm F, Auge N, Robinet C, Cambus JP, Parsons SJ, Salvayre R, Negre-Salvayre A: The sphingomyelin/ceramide pathway is involved in ERK1/2 phosphorylation, cell proliferation, and uPAR overexpression induced by tissue-type plasminogen activator. FASEB J. 2004 Sep;18(12):1398-400. Epub 2004 Jul 1. [PubMed:15231724]
  2. Bankl HC, Samorapoompichit P, Pikula B, Latinovic L, Bankl H, Lechner K, Valent P: Characterization of human prostate mast cells and their increase in periprostatic vein thrombosis. Am J Clin Pathol. 2001 Jul;116(1):97-106. [PubMed:11447759]
  3. Ferrier CM, Van Geloof WL, Straatman H, Van De Molengraft FJ, Van Muijen GN, Ruiter DJ: Spitz naevi may express components of the plasminogen activation system. J Pathol. 2002 Sep;198(1):92-9. [PubMed:12210068]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major con...
Gene Name
SERPINE1
Uniprot ID
P05121
Uniprot Name
Plasminogen activator inhibitor 1
Molecular Weight
45059.695 Da
References
  1. Lindberg P, Kinnby B, Lecander I, Lang NP, Matsson L: Increasing expression of tissue plasminogen activator and plasminogen activator inhibitor type 2 in dog gingival tissues with progressive inflammation. Arch Oral Biol. 2001 Jan;46(1):23-31. [PubMed:11163592]
  2. Hattori M, Azami Y: Searching for preventive measures of cardiovascular events in aged Japanese taxi drivers--the daily rhythm of cardiovascular risk factors during a night duty day. J Hum Ergol (Tokyo). 2001 Dec;30(1-2):321-6. [PubMed:14564902]
  3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Inhibits urokinase-type plasminogen activator. The monocyte derived PAI-2 is distinct from the endothelial cell-derived PAI-1.
Gene Name
SERPINB2
Uniprot ID
P05120
Uniprot Name
Plasminogen activator inhibitor 2
Molecular Weight
46595.84 Da
References
  1. Verkleij-Hagoort AC, Ursem NT, Hop WC, Geurts-Moespot A, Steegers EA, Sweep FC, Steegers-Theunissen RP: Complex congenital malformations and the impact of the plasminogen activator system and beta-hCG in amniotic fluid. Eur J Obstet Gynecol Reprod Biol. 2007 Nov;135(1):47-52. Epub 2006 Dec 1. [PubMed:17141398]
  2. Bremer HA, Brommer EJ, Wallenburg HC: Effects of labor and delivery on fibrinolysis. Eur J Obstet Gynecol Reprod Biol. 1994 Jun 30;55(3):163-8. [PubMed:7958159]
  3. Stump DC, Thienpont M, Collen D: Purification and characterization of a novel inhibitor of urokinase from human urine. Quantitation and preliminary characterization in plasma. J Biol Chem. 1986 Sep 25;261(27):12759-66. [PubMed:3091604]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Kringle domain binding
Specific Function
Tetranectin binds to plasminogen and to isolated kringle 4. May be involved in the packaging of molecules destined for exocytosis.
Gene Name
CLEC3B
Uniprot ID
P05452
Uniprot Name
Tetranectin
Molecular Weight
22536.665 Da
References
  1. Westergaard UB, Andersen MH, Heegaard CW, Fedosov SN, Petersen TE: Tetranectin binds hepatocyte growth factor and tissue-type plasminogen activator. Eur J Biochem. 2003 Apr;270(8):1850-4. [PubMed:12694198]
  2. Kamper EF, Kopeikina LT, Koutsoukos V, Stavridis J: Plasma tetranectin levels and disease activity in patients with rheumatoid arthritis. J Rheumatol. 1997 Feb;24(2):262-8. [PubMed:9034981]
  3. Vuckovic B, Deric M: [Lipoprotein(a): a link between thrombogenesis and atherogenesis]. Med Pregl. 2007 Jan-Feb;60(1-2):37-41. [PubMed:17853709]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Structural molecule activity
Specific Function
Together with KRT19, helps to link the contractile apparatus to dystrophin at the costameres of striated muscle.
Gene Name
KRT8
Uniprot ID
P05787
Uniprot Name
Keratin, type II cytoskeletal 8
Molecular Weight
53703.76 Da
References
  1. Kralovich KR, Li L, Hembrough TA, Webb DJ, Karns LR, Gonias SL: Characterization of the binding sites for plasminogen and tissue-type plasminogen activator in cytokeratin 8 and cytokeratin 18. J Protein Chem. 1998 Nov;17(8):845-54. [PubMed:9988531]
  2. Hembrough TA, Kralovich KR, Li L, Gonias SL: Cytokeratin 8 released by breast carcinoma cells in vitro binds plasminogen and tissue-type plasminogen activator and promotes plasminogen activation. Biochem J. 1996 Aug 1;317 ( Pt 3):763-9. [PubMed:8760360]
  3. Hembrough TA, Li L, Gonias SL: Cell-surface cytokeratin 8 is the major plasminogen receptor on breast cancer cells and is required for the accelerated activation of cell-associated plasminogen by tissue-type plasminogen activator. J Biol Chem. 1996 Oct 11;271(41):25684-91. [PubMed:8810346]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
S100 protein binding
Specific Function
Calcium-regulated membrane-binding protein whose affinity for calcium is greatly enhanced by anionic phospholipids. It binds two calcium ions with high affinity. May be involved in heat-stress resp...
Gene Name
ANXA2
Uniprot ID
P07355
Uniprot Name
Annexin A2
Molecular Weight
38603.63 Da
References
  1. Diaz VM, Hurtado M, Thomson TM, Reventos J, Paciucci R: Specific interaction of tissue-type plasminogen activator (t-PA) with annexin II on the membrane of pancreatic cancer cells activates plasminogen and promotes invasion in vitro. Gut. 2004 Jul;53(7):993-1000. [PubMed:15194650]
  2. Kang HM, Choi KS, Kassam G, Fitzpatrick SL, Kwon M, Waisman DM: Role of annexin II tetramer in plasminogen activation. Trends Cardiovasc Med. 1999 Apr-May;9(3-4):92-102. [PubMed:10578524]
  3. MacLeod TJ, Kwon M, Filipenko NR, Waisman DM: Phospholipid-associated annexin A2-S100A10 heterotetramer and its subunits: characterization of the interaction with tissue plasminogen activator, plasminogen, and plasmin. J Biol Chem. 2003 Jul 11;278(28):25577-84. Epub 2003 Apr 30. [PubMed:12730231]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Calcium-binding chaperone that promotes folding, oligomeric assembly and quality control in the endoplasmic reticulum (ER) via the calreticulin/calnexin cycle. This lectin interacts transiently wit...
Gene Name
CALR
Uniprot ID
P27797
Uniprot Name
Calreticulin
Molecular Weight
48141.2 Da
References
  1. Allen S, Bulleid NJ: Calnexin and calreticulin bind to enzymically active tissue-type plasminogen activator during biosynthesis and are not required for folding to the native conformation. Biochem J. 1997 Nov 15;328 ( Pt 1):113-9. [PubMed:9359841]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Poly(a) rna binding
Specific Function
Calcium-binding protein that interacts with newly synthesized glycoproteins in the endoplasmic reticulum. It may act in assisting protein assembly and/or in the retention within the ER of unassembl...
Gene Name
CANX
Uniprot ID
P27824
Uniprot Name
Calnexin
Molecular Weight
67567.695 Da
References
  1. Allen S, Bulleid NJ: Calnexin and calreticulin bind to enzymically active tissue-type plasminogen activator during biosynthesis and are not required for folding to the native conformation. Biochem J. 1997 Nov 15;328 ( Pt 1):113-9. [PubMed:9359841]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Receptor activity
Specific Function
Endocytic receptor involved in endocytosis and in phagocytosis of apoptotic cells. Required for early embryonic development. Involved in cellular lipid homeostasis. Involved in the plasma clearance...
Gene Name
LRP1
Uniprot ID
Q07954
Uniprot Name
Prolow-density lipoprotein receptor-related protein 1
Molecular Weight
504601.695 Da
References
  1. Moestrup SK, Nielsen S, Andreasen P, Jorgensen KE, Nykjaer A, Roigaard H, Gliemann J, Christensen EI: Epithelial glycoprotein-330 mediates endocytosis of plasminogen activator-plasminogen activator inhibitor type-1 complexes. J Biol Chem. 1993 Aug 5;268(22):16564-70. [PubMed:8344937]
  2. Nykjaer A, Petersen CM, Moller B, Jensen PH, Moestrup SK, Holtet TL, Etzerodt M, Thogersen HC, Munch M, Andreasen PA, et al.: Purified alpha 2-macroglobulin receptor/LDL receptor-related protein binds urokinase.plasminogen activator inhibitor type-1 complex. Evidence that the alpha 2-macroglobulin receptor mediates cellular degradation of urokinase receptor-bound complexes. J Biol Chem. 1992 Jul 25;267(21):14543-6. [PubMed:1378833]
  3. Hu K, Yang J, Tanaka S, Gonias SL, Mars WM, Liu Y: Tissue-type plasminogen activator acts as a cytokine that triggers intracellular signal transduction and induces matrix metalloproteinase-9 gene expression. J Biol Chem. 2006 Jan 27;281(4):2120-7. Epub 2005 Nov 22. [PubMed:16303771]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2017 09:34