Identification

Name
Urokinase
Accession Number
DB00013  (BTD00030, BIOD00030)
Type
Biotech
Groups
Approved, Investigational, Withdrawn
Biologic Classification
Protein Based Therapies
Blood factors
Description

Urokinase is an endogenous peptide that is cleaved in the presence of plasmin between lysine 158 and isoleucine 159 to yield active urokinase.2 Urokinase remains connected between these 2 chains by a sulfhydryl bond.2

Urokinase was granted FDA approval on 16 January 1978.3

Protein structure
Db00013
Protein chemical formula
C1376H2145N383O406S18
Protein average weight
31126.5 Da
Sequences
>DB00013 sequence
KPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLMS
PCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHND
IALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMT
VVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVS
WGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
Download FASTA Format
Synonyms
  • Kinase (enzyme-activating), uro-urokinase
  • TCUK
  • Tissue culture urokinase
  • Two-chain urokinase
  • Urochinasi
  • Urokinase
  • Urokinasum
  • Uroquinasa
External IDs
WIN 22005
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
KinlyticInjection, powder, lyophilized, for solution250000 [iU]/5mLIntravenousImaRx Therapeutics, Inc.2007-06-08Not applicableUs
Kinlytic (urokinase for Injection)Powder, for solutionIntravenousMicrobix Biosystems Inc1988-12-312009-10-28Canada
Kinlytic Open-cathPowder, for solutionIntravenousMicrobix Biosystems Inc1991-12-312009-10-28Canada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
Abbokinase (Abbott Laboratories)
Categories
UNII
83G67E21XI
CAS number
9039-53-6

Pharmacology

Indication

In Canada, urokinase is indicated for lysis of acute massive pulmonary emboli, acute thrombi obstructing coronary arteries, occlusive thromboemboli in peripheral arteries and grafts, and restoration of patency to intravenous catheters.4

Associated Conditions
Pharmacodynamics

Urokinase is a serine protease that activates plasminogen to an active fibrinolytic protease.1 The duration of action is short due to the short half life.3 Patients should be counselled regarding the risk of bleeding, anaphylaxis, infusion reactions, and cholesterol embolization.[L12138

Mechanism of action

Urokinase is a serine protease.1 It cleaves plasminogen to form the active fibrinolytic protease, plasmin.1

TargetActionsOrganism
APlasminogen
activator
Humans
AUrokinase plasminogen activator surface receptor
inducer
modulator
Humans
APlasminogen activator inhibitor 1
substrate
inducer
Humans
APlasminogen activator inhibitor 2
substrate
inducer
Humans
UPlasma serine protease inhibitor
substrate
Humans
ULow-density lipoprotein receptor-related protein 2
substrate
Humans
USuppressor of tumorigenicity 14 protein
substrate
Humans
UNidogen-1
ligand
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Urokinase is delivered intravenously, so the bioavailability is high.

Volume of distribution

The volume of distribution of urokinase is 11.5L.3

Protein binding

Data regarding the protein binding of urokinase in plasma is not readily available.

Metabolism

Because urokinase is a protein, it is expected to be metabolized by proteases to smaller proteins and amino acids.

Route of elimination

Urokinase is eliminated in the bile and urine.3

Half life

Urokinase has a half life of 12.6±6.2 minutes.3

Clearance

Data regarding the clearance of urokinase is not readily available.

Toxicity

Patients experiencing an overdose may present with bleeding.4 Treat patients with symptomatic and supportive measures which may include application of local pressure, administration of whole blood or plasma, and administration of aminocaproic acid.4

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Urokinase Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(1,2,6,7-3H)Testosterone(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Urokinase.
(R)-warfarinUrokinase may increase the anticoagulant activities of (R)-warfarin.
(S)-WarfarinUrokinase may increase the anticoagulant activities of (S)-Warfarin.
1-Testosterone1-Testosterone may increase the anticoagulant activities of Urokinase.
18-methyl-19-nortestosterone18-methyl-19-nortestosterone may increase the anticoagulant activities of Urokinase.
3,5-Diiodotyrosine3,5-Diiodotyrosine may increase the anticoagulant activities of Urokinase.
4-hydroxycoumarinUrokinase may increase the anticoagulant activities of 4-hydroxycoumarin.
4-Hydroxytestosterone4-Hydroxytestosterone may increase the anticoagulant activities of Urokinase.
5beta-dihydrotestosterone5beta-dihydrotestosterone may increase the anticoagulant activities of Urokinase.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Urokinase.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

References

Synthesis Reference

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

US4258030
General References
  1. Urano T, Castellino FJ, Suzuki Y: Regulation of plasminogen activation on cell surfaces and fibrin. J Thromb Haemost. 2018 May 20. doi: 10.1111/jth.14157. [PubMed:29779246]
  2. Kasai S, Arimura H, Nishida M, Suyama T: Primary structure of single-chain pro-urokinase. J Biol Chem. 1985 Oct 5;260(22):12382-9. [PubMed:2931434]
  3. FDA Approved Drug Products: Kinlytic Urokinase Injection (Discontinued) [Link]
  4. Health Canada Approved Drug Products: Urokinase Injection [Link]
External Links
UniProt
P00749
Genbank
X02419
PubChem Substance
46506299
RxNav
11055
ChEMBL
CHEMBL1201420
Therapeutic Targets Database
DAP001194
PharmGKB
PA451836
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Urokinase
ATC Codes
B01AD04 — Urokinase

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentEmpyema1
2CompletedTreatmentAcute Peripheral Arterial Occlusion1
2CompletedTreatmentArterial Occlusive Diseases / Diabetic Foot / Ischaemia1
2CompletedTreatmentFallopian Tube Carcinoma / Malignant Ovarian Mixed Epithelial Tumor / Ovarian Brenner Tumor / Ovarian Clear Cell Cystadenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mucinous Cystadenocarcinoma / Ovarian Serous Cystadenocarcinoma / Primary Peritoneal Carcinoma / Recurrent Ovarian Carcinoma / Undifferentiated Ovarian Carcinoma1
2RecruitingTreatmentStroke, Ischemic1
2, 3TerminatedTreatmentSinus Thrombosis, Intracranial1
2, 3Unknown StatusTreatmentPleural Empyema1
3CompletedTreatmentAcute Ischaemic Stroke2
3CompletedTreatmentEmpyema / Pneumonia1
3CompletedTreatmentInfection / Patency1
3Not Yet RecruitingTreatmentMinor Stroke1
3RecruitingTreatmentPleural Empyema1
3TerminatedTreatmentArterial Occlusive Diseases / Diabetic Foot / Ischaemia1
3TerminatedTreatmentCritical Limb Ischemia (CLI) / Diabetic Foot1
3Unknown StatusTreatmentRetained Hemothorax1
4CompletedTreatmentPleural Diseases / Pleural Effusions / Pleural Empyema1
4CompletedTreatmentPulmonary Embolism / Pulmonary Thromboembolism1
4CompletedTreatmentPulmonary Embolism / Thromboembolism1
4Enrolling by InvitationTreatmentCoronary Artery Disease (CAD)1
Not AvailableCompletedNot AvailableStroke, Ischemic1
Not AvailableEnrolling by InvitationTreatmentThrombosis, Venous1
Not AvailableWithdrawnNot AvailableStroke, Ischemic1

Pharmacoeconomics

Manufacturers
  • Microbix biosystems inc
Packagers
  • Hospira Inc.
  • ImaRx Therapeutics
  • Microbix Biosystems Inc.
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous250000 [iU]/5mL
Powder, for solutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)76 °C at pH 4.5Nowak, U.K. et al., Biochemistry 33:2951-2960 (1994)
hydrophobicity-0.466Not Available
isoelectric point8.66Not 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
Humans
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. 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]
  7. FDA Approved Drug Products: Kinlytic Urokinase Injection (Discontinued) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inducer
Modulator
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. 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
Humans
Pharmacological action
Yes
Actions
Substrate
Inducer
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. 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
Humans
Pharmacological action
Yes
Actions
Substrate
Inducer
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. 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
Humans
Pharmacological action
Unknown
Actions
Substrate
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...
Gene Name
SERPINA5
Uniprot ID
P05154
Uniprot Name
Plasma serine protease inhibitor
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
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Low-density lipoprotein receptor-related protein 2 mediates endocytosis of urokinase.
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
Uniprot Name
Low-density lipoprotein receptor-related protein 2
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
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Suppressor of tumorigenicity 14 protein activates urokinase.
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...
Gene Name
ST14
Uniprot ID
Q9Y5Y6
Uniprot Name
Suppressor of tumorigenicity 14 protein
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
Humans
Pharmacological action
Unknown
Actions
Ligand
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 inter...
Gene Name
NID1
Uniprot ID
P14543
Uniprot Name
Nidogen-1
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]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
May be involved in tissue injury and remodeling. Has significant elastolytic activity. Can accept large and small amino acids at the P1' site, but has a preference for leucine. Aromatic or hydropho...
Gene Name
MMP12
Uniprot ID
P39900
Uniprot Name
Macrophage metalloelastase
Molecular Weight
54001.175 Da
References
  1. Andolfo A, English WR, Resnati M, Murphy G, Blasi F, Sidenius N: Metalloproteases cleave the urokinase-type plasminogen activator receptor in the D1-D2 linker region and expose epitopes not present in the intact soluble receptor. Thromb Haemost. 2002 Aug;88(2):298-306. [PubMed:12195704]

Drug created on June 13, 2005 07:24 / Updated on July 10, 2020 21:42

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