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Identification
NameUrokinase
Accession NumberDB00013  (BTD00030, BIOD00030)
TypeBiotech
GroupsApproved, Investigational, Withdrawn
DescriptionLow molecular weight form of human urokinase, that consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. Recombinant urokinase plasminogen activator
Protein structureDb00013
Related Articles
Protein chemical formulaC1376H2145N383O406S18
Protein average weight31126.5 Da
Sequences
>DB00013 sequence
KPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLMS
PCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHND
IALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMT
VVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVS
WGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
Download FASTA Format
Synonyms
U-plasminogen activator
uPA
Urokinase-type plasminogen activator precursor
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Kinlytic (urokinase for Injection)Powder, for solution250000 unitIntravenousMicrobix Biosystems Inc1988-12-312009-10-28Canada
Kinlytic Open-cathPowder, for solution5000 unitIntravenousMicrobix Biosystems Inc1991-12-312009-10-28Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AbbokinaseAbbott Laboratories
KinlyticMicrobix Biosystems Inc.
Brand mixturesNot Available
SaltsNot Available
Categories
UNII83G67E21XI
CAS number9039-53-6
Pharmacology
IndicationUrokinase can be used for the treatment of pulminary embolism, coronary artery thrombosis, IV catheter clearance, and venous and arterial blood clots.
Structured Indications Not Available
PharmacodynamicsUrokinase is used for the treatment of pulmonary embolisms. The low molecular weight form of human urokinase consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. Urokinase is an enzyme (protein) produced by the kidney, and found in the urine. There are two forms of urokinase which differ in molecular weight but have similar clinical effects. Urokinase is the low molecular weight form. Urokinase acts on the endogenous fibrinolytic system. It converts plasminogen to the enzyme plasmin. Plasmin degrades fibrin clots as well as fibrinogen and some other plasma proteins.
Mechanism of actionUrokinase acts on the endogenous fibrinolytic system. It cleaves the Arg-Val bond in plasminogen to produce active plasmin. Plasmin degrades fibrin clots as well as fibrinogen and other plasma proteins.
TargetKindPharmacological actionActionsOrganismUniProt ID
PlasminogenProteinyes
activator
HumanP00747 details
Urokinase plasminogen activator surface receptorProteinyesNot AvailableHumanQ03405 details
Urokinase-type plasminogen activatorProteinyesNot AvailableHumanP00749 details
Tissue-type plasminogen activatorProteinyesNot AvailableHumanP00750 details
Plasminogen activator inhibitor 1ProteinyesNot AvailableHumanP05121 details
Plasminogen activator inhibitor 2ProteinyesNot AvailableHumanP05120 details
Plasma serine protease inhibitorProteinunknownNot AvailableHumanP05154 details
Low-density lipoprotein receptor-related protein 2ProteinunknownNot AvailableHumanP98164 details
Suppressor of tumorigenicity 14 proteinProteinunknownNot AvailableHumanQ9Y5Y6 details
Nidogen-1ProteinunknownNot AvailableHumanP14543 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Proteolysis

Route of eliminationUrokinase administered by intravenous infusion is rapidly cleared by the liver. Small fractions of the administered dose are excreted in bile and urine
Half life12 minutes. Small fractions of the administered dose are excreted in bile and urine
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Urokinase Action PathwayDrug actionSMP00284
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabUrokinase may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolUrokinase may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Urokinase.Approved, Vet Approved
AlprostadilAlprostadil may increase the anticoagulant activities of Urokinase.Approved, Investigational
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Urokinase.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Urokinase.Approved
AncrodUrokinase may increase the anticoagulant activities of Ancrod.Investigational
Antithrombin III humanUrokinase may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanUrokinase may increase the anticoagulant activities of Apixaban.Approved
AprotininThe therapeutic efficacy of Urokinase can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinUrokinase may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanUrokinase may increase the anticoagulant activities of Argatroban.Approved, Investigational
AzelastineAzelastine may increase the anticoagulant activities of Urokinase.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Urokinase.Approved, Investigational
BecaplerminUrokinase may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BeraprostBeraprost may increase the anticoagulant activities of Urokinase.Investigational
BivalirudinUrokinase may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
ButylphthalideButylphthalide may increase the anticoagulant activities of Urokinase.Investigational
CangrelorCangrelor may increase the anticoagulant activities of Urokinase.Approved
CertoparinUrokinase may increase the anticoagulant activities of Certoparin.Approved
CilostazolCilostazol may increase the anticoagulant activities of Urokinase.Approved
Citric AcidUrokinase may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Urokinase.Approved, Nutraceutical
Dabigatran etexilateUrokinase may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinUrokinase may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidUrokinase may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DefibrotideDefibrotide may increase the anticoagulant activities of Urokinase.Approved, Investigational
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Urokinase.Investigational
DesirudinUrokinase may increase the anticoagulant activities of Desirudin.Approved
DextranUrokinase may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Urokinase may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Urokinase may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Urokinase may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolUrokinase may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Urokinase.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Urokinase.Approved
Edetic AcidUrokinase may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanUrokinase may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinUrokinase may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Urokinase.Approved, Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Urokinase.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Urokinase.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Urokinase.Approved, Investigational
Ethyl biscoumacetateUrokinase may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FluindioneUrokinase may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxUrokinase may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumUrokinase may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateUrokinase may increase the anticoagulant activities of Gabexate.Investigational
HeparinUrokinase may increase the anticoagulant activities of Heparin.Approved, Investigational
HirulogUrokinase may increase the anticoagulant activities of Hirulog.Experimental
IbudilastIbudilast may increase the anticoagulant activities of Urokinase.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Urokinase.Approved, Nutraceutical
idraparinuxUrokinase may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Urokinase.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Urokinase.Approved, Investigational
KetanserinKetanserin may increase the anticoagulant activities of Urokinase.Investigational
LepirudinUrokinase may increase the anticoagulant activities of Lepirudin.Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Urokinase.Approved
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Urokinase.Approved
MilrinoneMilrinone may increase the anticoagulant activities of Urokinase.Approved
NadroparinUrokinase may increase the anticoagulant activities of Nadroparin.Approved
NafamostatUrokinase may increase the anticoagulant activities of Nafamostat.Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Urokinase.Investigational
NCX 4016NCX 4016 may increase the anticoagulant activities of Urokinase.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Urokinase.Approved, Withdrawn
NitroaspirinNitroaspirin may increase the anticoagulant activities of Urokinase.Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Urokinase.Approved
OtamixabanUrokinase may increase the anticoagulant activities of Otamixaban.Investigational
Pentosan PolysulfateUrokinase may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Urokinase.Approved, Investigational
PhenindioneUrokinase may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonUrokinase may increase the anticoagulant activities of Phenprocoumon.Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Urokinase.Approved
Protein CUrokinase may increase the anticoagulant activities of Protein C.Approved
Protein S humanUrokinase may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeUrokinase may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Urokinase.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Urokinase.Experimental, Investigational
ReviparinUrokinase may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Urokinase.Approved
RivaroxabanUrokinase 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 Urokinase.Approved, Vet Approved
SCH-530348SCH-530348 may increase the anticoagulant activities of Urokinase.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Urokinase.Approved, Vet Approved
SRT501SRT501 may increase the anticoagulant activities of Urokinase.Investigational
SulodexideUrokinase may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TesmilifeneTesmilifene may increase the anticoagulant activities of Urokinase.Investigational
TiclopidineTiclopidine may increase the anticoagulant activities of Urokinase.Approved
TirofibanTirofiban may increase the anticoagulant activities of Urokinase.Approved
TranilastTranilast may increase the anticoagulant activities of Urokinase.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Urokinase.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Urokinase is combined with Treprostinil.Approved, Investigational
TriflusalTriflusal may increase the anticoagulant activities of Urokinase.Approved
VorapaxarVorapaxar may increase the anticoagulant activities of Urokinase.Approved
WarfarinUrokinase may increase the anticoagulant activities of Warfarin.Approved
XimelagatranUrokinase may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Urokinase may increase the anticoagulant activities of Ym150.Investigational
Food InteractionsNot Available
References
Synthesis Reference

Koji Sasaki, Yasukazu Harada, “Urokinase preparation for oral administration.” U.S. Patent US4258030, issued November, 1975.

US4258030
General References
  1. Housley C: Contract purchasing means a buyer's market. Dimens Health Serv. 1976 Apr;53(4):16, 19-20. [PubMed:5328 ]
External Links
ATC CodesB01AD04
AHFS Codes
  • 20:12.20
PDB Entries
FDA labelNot Available
MSDSNot Available
Pharmacoeconomics
Manufacturers
  • Microbix biosystems inc
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous250000 unit
Powder, for solutionIntravenous5000 unit
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point76 °C at pH 4.5Nowak, U.K. et al., Biochemistry 33:2951-2960 (1994)
hydrophobicity-0.466Not Available
isoelectric point8.66Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot 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 ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin ...
Gene Name:
PLG
Uniprot ID:
P00747
Molecular Weight:
90568.415 Da
References
  1. Zhang X, Zhou H, Shen G, Liu Z, Hu Y, Wei W, Song S: Study on the mechanism of the annexin II-mediated co-assembly of t-PA and plasminogen. J Huazhong Univ Sci Technolog Med Sci. 2002;22(1):21-3, 76. [PubMed:12658774 ]
  2. Lopez-Alemany R, Longstaff C, Hawley S, Mirshahi M, Fabregas P, Jardi M, Merton E, Miles LA, Felez J: Inhibition of cell surface mediated plasminogen activation by a monoclonal antibody against alpha-Enolase. Am J Hematol. 2003 Apr;72(4):234-42. [PubMed:12666133 ]
  3. Hashimoto M, Oiwa K, Matsuo O, Ueshima S, Okada K, Okada Y, Okamoto S, Giddings JC, Yamamoto J: Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model. Thromb Haemost. 2003 May;89(5):820-5. [PubMed:12719778 ]
  4. Guda K, Claffey KP, Dong M, Nambiar PR, Rosenberg DW: Defective processing of the transforming growth factor-beta1 in azoxymethane-induced mouse colon tumors. Mol Carcinog. 2003 May;37(1):51-9. [PubMed:12720300 ]
  5. Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47. [PubMed:12745435 ]
  6. 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:
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-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.
Gene Name:
PLAUR
Uniprot ID:
Q03405
Molecular Weight:
36977.62 Da
References
  1. Czekay RP, Aertgeerts K, Curriden SA, Loskutoff DJ: Plasminogen activator inhibitor-1 detaches cells from extracellular matrices by inactivating integrins. J Cell Biol. 2003 Mar 3;160(5):781-91. [PubMed:12615913 ]
  2. Fuchs T, Allgayer H: Transcriptional regulation of the urokinase receptor (u-PAR)--a central molecule of invasion and metastasis. Biol Chem. 2003 May;384(5):755-61. [PubMed:12817472 ]
  3. Kanse SM, Chavakis T, Al-Fakhri N, Hersemeyer K, Monard D, Preissner KT: Reciprocal regulation of urokinase receptor (CD87)-mediated cell adhesion by plasminogen activator inhibitor-1 and protease nexin-1. J Cell Sci. 2004 Jan 26;117(Pt 3):477-85. Epub 2003 Dec 16. [PubMed:14679304 ]
  4. Beaufort N, Leduc D, Rousselle JC, Magdolen V, Luther T, Namane A, Chignard M, Pidard D: Proteolytic regulation of the urokinase receptor/CD87 on monocytic cells by neutrophil elastase and cathepsin G. J Immunol. 2004 Jan 1;172(1):540-9. [PubMed:14688365 ]
  5. Guerrero J, Santibanez JF, Gonzalez A, Martinez J: EGF receptor transactivation by urokinase receptor stimulus through a mechanism involving Src and matrix metalloproteinases. Exp Cell Res. 2004 Jan 1;292(1):201-8. [PubMed:14720519 ]
  6. Gutova M, Najbauer J, Gevorgyan A, Metz MZ, Weng Y, Shih CC, Aboody KS: Identification of uPAR-positive chemoresistant cells in small cell lung cancer. PLoS One. 2007 Feb 28;2(2):e243. [PubMed:17327908 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Serine-type endopeptidase activity
Specific Function:
Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
Gene Name:
PLAU
Uniprot ID:
P00749
Molecular Weight:
48507.09 Da
References
  1. Bell WR: Present-day thrombolytic therapy: therapeutic agents--pharmacokinetics and pharmacodynamics. Rev Cardiovasc Med. 2002;3 Suppl 2:S34-44. [PubMed:12556741 ]
  2. Gamberi G, Serra M, Ragazzini P, Magagnoli G, Pazzaglia L, Ponticelli F, Ferrari C, Zanasi M, Bertoni F, Picci P, Benassi MS: Identification of markers of possible prognostic value in 57 giant cell tumors of bone. Oncol Rep. 2003 Mar-Apr;10(2):351-6. [PubMed:12579271 ]
  3. Zhang G, Kim H, Cai X, Lopez-Guisa JM, Alpers CE, Liu Y, Carmeliet P, Eddy AA: Urokinase receptor deficiency accelerates renal fibrosis in obstructive nephropathy. J Am Soc Nephrol. 2003 May;14(5):1254-71. [PubMed:12707394 ]
  4. Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47. [PubMed:12745435 ]
  5. Wielockx B, Libert C: Serine proteases of the fibrinolysis pathway are not involved in lethal hepatitis and fibrinogen breakdown induced by tumor necrosis factor. Cytokine. 2003 Mar 21;21(6):281-5. [PubMed:12824001 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Serine-type endopeptidase activity
Specific Function:
Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a single Arg-Val bond in plasminogen. By controlling plasmin-mediated proteolysis, it plays an important role in tissue remodeling and degradation, in cell migration and many other physiopathological events. Plays a direct role in facilitating neuronal migration.
Gene Name:
PLAT
Uniprot ID:
P00750
Molecular Weight:
62916.495 Da
References
  1. Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47. [PubMed:12745435 ]
  2. Lindholt JS, Jorgensen B, Shi GP, Henneberg EW: Relationships between activators and inhibitors of plasminogen, and the progression of small abdominal aortic aneurysms. Eur J Vasc Endovasc Surg. 2003 Jun;25(6):546-51. [PubMed:12787697 ]
  3. Aleman C, Alegre J, Monasterio J, Segura RM, Armadans L, Angles A, Varela E, Ruiz E, Fernandez de Sevilla T: Association between inflammatory mediators and the fibrinolysis system in infectious pleural effusions. Clin Sci (Lond). 2003 Nov;105(5):601-7. [PubMed:12826021 ]
  4. Wells RG, Havens PL: Intrapleural fibrinolysis for parapneumonic effusion and empyema in children. Radiology. 2003 Aug;228(2):370-8. [PubMed:12893898 ]
  5. Stief TW, Bunder R, Richter A, Maisch B, Renz H, Fareed J: In vitro simulation of therapeutic plasmatic fibrinolysis. Clin Appl Thromb Hemost. 2003 Jul;9(3):211-20. [PubMed:14507109 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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 control point in the regulation of fibrinolysis.
Gene Name:
SERPINE1
Uniprot ID:
P05121
Molecular Weight:
45059.695 Da
References
  1. Gamberi G, Serra M, Ragazzini P, Magagnoli G, Pazzaglia L, Ponticelli F, Ferrari C, Zanasi M, Bertoni F, Picci P, Benassi MS: Identification of markers of possible prognostic value in 57 giant cell tumors of bone. Oncol Rep. 2003 Mar-Apr;10(2):351-6. [PubMed:12579271 ]
  2. Shetty S, Bdeir K, Cines DB, Idell S: Induction of plasminogen activator inhibitor-1 by urokinase in lung epithelial cells. J Biol Chem. 2003 May 16;278(20):18124-31. Epub 2003 Mar 17. [PubMed:12642587 ]
  3. Hellgren M: Hemostasis during normal pregnancy and puerperium. Semin Thromb Hemost. 2003 Apr;29(2):125-30. [PubMed:12709915 ]
  4. Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47. [PubMed:12745435 ]
  5. Gerstein ES, Shcherbakov AM, Kaz'min AI, Ognerubov NA, Kushlinskii NE: [Urokinase and tissue type plasminogen activators and their type-1 inhibitor (PAI-1) in gastric cancer]. Vopr Onkol. 2003;49(2):165-9. [PubMed:12785198 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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
Molecular Weight:
46595.84 Da
References
  1. Swartz JM, Bystrom J, Dyer KD, Nitto T, Wynn TA, Rosenberg HF: Plasminogen activator inhibitor-2 (PAI-2) in eosinophilic leukocytes. J Leukoc Biol. 2004 Oct;76(4):812-9. Epub 2004 Jul 26. [PubMed:15277569 ]
  2. Wygrecka M, Markart P, Ruppert C, Kuchenbuch T, Fink L, Bohle RM, Grimminger F, Seeger W, Gunther A: Compartment- and cell-specific expression of coagulation and fibrinolysis factors in the murine lung undergoing inhalational versus intravenous endotoxin application. Thromb Haemost. 2004 Sep;92(3):529-40. [PubMed:15351849 ]
  3. Iglesias D, Alegre J, Aleman C, Ruiz E, Soriano T, Armadans LI, Segura RM, Angles A, Monasterio J, de Sevilla TF: Metalloproteinases and tissue inhibitors of metalloproteinases in exudative pleural effusions. Eur Respir J. 2005 Jan;25(1):104-9. [PubMed:15640330 ]
  4. Grebenchtchikov N, Maguire TM, Riisbro R, Geurts-Moespot A, O'Donovan N, Schmitt M, McGreal G, McDermott E, O'Higgins N, Brunner N, Sweep CG, Duffy MJ: Measurement of plasminogen activator system components in plasma and tumor tissue extracts obtained from patients with breast cancer: an EORTC Receptor and Biomarker Group collaboration. Oncol Rep. 2005 Jul;14(1):235-9. [PubMed:15944795 ]
  5. Fernandez-Soria V, Lleonart ME, Diaz-Fuertes M, Villuendas R, Sanchez-Prieto R, Fabra A, Ramon Y Cajal S: Adenovirus E1A orchestrates the urokinase-plasminogen activator system and upregulates PAI-2 expression, supporting a tumor suppressor effect. Int J Oncol. 2006 Jan;28(1):143-8. [PubMed:16327990 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Heparin-dependent serine protease inhibitor acting in body fluids and secretions. Inactivates serine proteases by binding irreversibly to their serine activation site. Involved in the regulation of intravascular and extravascular proteolytic activities. Plays hemostatic roles in the blood plasma. Acts as a procoagulant and proinflammatory factor by inhibiting the anticoagulant activated protein...
Gene Name:
SERPINA5
Uniprot ID:
P05154
Molecular Weight:
45674.315 Da
References
  1. Uhrin P, Schofer C, Zaujec J, Ryban L, Hilpert M, Weipoltshammer K, Jerabek I, Pirtzkall I, Furtmuller M, Dewerchin M, Binder BR, Geiger M: Male fertility and protein C inhibitor/plasminogen activator inhibitor-3 (PCI): localization of PCI in mouse testis and failure of single plasminogen activator knockout to restore spermatogenesis in PCI-deficient mice. Fertil Steril. 2007 Oct;88(4 Suppl):1049-57. Epub 2007 Apr 16. [PubMed:17434507 ]
  2. Espana F, Navarro S, Medina P, Zorio E, Estelles A: The role of protein C inhibitor in human reproduction. Semin Thromb Hemost. 2007 Feb;33(1):41-5. [PubMed:17253188 ]
  3. Odet F, Guyot R, Leduque P, Le Magueresse-Battistoni B: Evidence for similar expression of protein C inhibitor and the urokinase-type plasminogen activator system during mouse testis development. Endocrinology. 2004 Mar;145(3):1481-9. Epub 2003 Nov 26. [PubMed:14645112 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Calcium ion binding
Specific Function:
Acts together with cubilin to mediate HDL endocytosis (By similarity). May participate in regulation of parathyroid-hormone and para-thyroid-hormone-related protein release.
Gene Name:
LRP2
Uniprot ID:
P98164
Molecular Weight:
521952.77 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Kanalas JJ: Effect of the nephritogenic autoantibody of Heymann's nephritis on plasminogen-binding to gp330 and activation by urokinase. Biochim Biophys Acta. 1993 Nov 25;1225(1):101-6. [PubMed:8241286 ]
  4. Kanalas JJ: Analysis of plasmin binding and urokinase activation of plasminogen bound to the Heymann nephritis autoantigen, gp330. Arch Biochem Biophys. 1992 Dec;299(2):255-60. [PubMed:1280065 ]
  5. Korenberg JR, Argraves KM, Chen XN, Tran H, Strickland DK, Argraves WS: Chromosomal localization of human genes for the LDL receptor family member glycoprotein 330 (LRP2) and its associated protein RAP (LRPAP1). Genomics. 1994 Jul 1;22(1):88-93. [PubMed:7959795 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type peptidase activity
Specific Function:
Degrades extracellular matrix. Proposed to play a role in breast cancer invasion and metastasis. Exhibits trypsin-like activity as defined by cleavage of synthetic substrates with Arg or Lys as the P1 site. Involved in the terminal differentiation of keratinocytes through prostasin (PRSS8) activation and filaggrin (FLG) processing.
Gene Name:
ST14
Uniprot ID:
Q9Y5Y6
Molecular Weight:
94769.01 Da
References
  1. Suzuki M, Kobayashi H, Kanayama N, Saga Y, Suzuki M, Lin CY, Dickson RB, Terao T: Inhibition of tumor invasion by genomic down-regulation of matriptase through suppression of activation of receptor-bound pro-urokinase. J Biol Chem. 2004 Apr 9;279(15):14899-908. Epub 2004 Jan 27. [PubMed:14747469 ]
  2. Kirchhofer D, Peek M, Li W, Stamos J, Eigenbrot C, Kadkhodayan S, Elliott JM, Corpuz RT, Lazarus RA, Moran P: Tissue expression, protease specificity, and Kunitz domain functions of hepatocyte growth factor activator inhibitor-1B (HAI-1B), a new splice variant of HAI-1. J Biol Chem. 2003 Sep 19;278(38):36341-9. Epub 2003 Jun 18. [PubMed:12815039 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Proteoglycan binding
Specific Function:
Sulfated glycoprotein widely distributed in basement membranes and tightly associated with laminin. Also binds to collagen IV and perlecan. It probably has a role in cell-extracellular matrix interactions.
Gene Name:
NID1
Uniprot ID:
P14543
Molecular Weight:
136375.93 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Stephens RW, Aumailley M, Timpl R, Reisberg T, Tapiovaara H, Myohanen H, Murphy-Ullrich J, Vaheri A: Urokinase binding to laminin-nidogen. Structural requirements and interactions with heparin. Eur J Biochem. 1992 Aug 1;207(3):937-42. [PubMed:1499567 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23