Therapeutic Targets Database
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TTD Target ID: TTDS00392

Target Information
NamePlasminogen    
Type of targetSuccessful target    
SynonymsPLG    
Plasmin    
DiseaseExcessive postoperative bleeding    [1][2]
Hemorrhage    [1][2]
Drug(s)AlteplaseApprovedPulmonary embolism[3]
Aminocaproic AcidApprovedExcessive postoperative bleeding[1][2]
AnistreplaseApprovedAcute Coronary thrombosis[4][5]
ReteplaseApprovedHeart attack[6][7]
StreptokinaseApprovedPulmonary embolism [8]
TenecteplaseApprovedMyocardial infarction[3]
Tranexamic AcidApprovedExcessive bleeding[9]
UrokinaseApprovedDeep venous thrombosis; Pulmonary embolism; Myocardial infarction; Occluded intravenous or dialysis cannulas[10]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.21.7
PathwayComplement and coagulation cascades
Neuroactive ligand-receptor interaction
UniProt IDP00747
PDB Structure1B2I; 1BML; 1BUI; 1CEA; 1CEB; 1DDJ; 1HPJ; 1HPK.    
SequenceMEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFT CRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKN GITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILE CEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRE LRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWS AQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTE QLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAG LTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEED CMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGG PWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRT RFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLE PTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQ LPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSW GLGCARPNKPGVYVRVSRFVTWIEGVMRNN
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- (2-Oxo-2-p-tolyl-ethyl)-1H-indole-2,3-dione[11]
1- (3,3-Dimethyl-2-oxo-butyl)-1H-indole-2,3-dione[11]
1-guanidino-7-isoquinolinesulphonamide[12]
1-guanidino-N-phenyl-7-isoquinolinesulphonamide[12]
2- (2-Hydroxy-phenyl)-1H-indole-5-carboxamidine[13]
Aminocaproic Acid[1][2]
Bicine[14]
GRASSYSTATIN A[15]
MELAGATRAN[16]
N- (4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine[17]
Tranexamic Acid[9]
ActivatorAlteplase[3]
Anistreplase[4][5]
Reteplase[6][7]
Streptokinase[8]
Tenecteplase[3]
Urokinase[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The blockage of the high-affinity lysine binding sites of plasminogen by EACA significantly inhibits prourokinase-induced plasminogen activation. Biochim Biophys Acta. 2002 Apr 29;1596(2):182-92. To Reference
Ref 2Analysis of plasmin binding and urokinase activation of plasminogen bound to the Heymann nephritis autoantigen, gp330. Arch Biochem Biophys. 1992 Dec;299(2):255-60. To Reference
Ref 3Thrombolytic therapies: the current state of affairs. J Endovasc Ther. 2005 Apr;12(2):224-32. To Reference
Ref 4Evaluation of thrombolytic agents. Drugs. 1997;54 Suppl 3:11-6; discussion 16-7. To Reference
Ref 5Therapeutic management of acute myocardial infarction. Am J Hosp Pharm. 1990 Sep;47(9 Suppl 2):S5-10. To Reference
Ref 6Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. To Reference
Ref 7Spotlight on reteplase in thrombotic occlusive disorders. BioDrugs. 2007;21(1):65-8. To Reference
Ref 8Acute anuric renal failure with streptokinase therapy in a patient with acute venous thromboembolic disease and the review of renal side effects of streptokinase. Tuberk Toraks. 2008;56(4):456-61. To Reference
Ref 9Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31. To Reference
Ref 10Deep vein thrombosis resolution is impaired in diet-induced type 2 diabetic mice. J Vasc Surg. 2008 Dec;48(6):1575-84. Epub 2008 Oct 1. To Reference
Ref 11Bioorg Med Chem Lett. 2000 Nov 20;10(22):2501-4.Parallel synthesis of isatin-based serine protease inhibitors. To Reference
Ref 12J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. To Reference
Ref 13J Med Chem. 2001 Aug 16;44(17):2753-71.Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. To Reference
Ref 14Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 15J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. To Reference
Ref 16Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. To Reference
Ref 17Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. To Reference



 

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