Target Information
Target General Infomation | |||||
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Target ID |
T89034
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Former ID |
TTDS00392
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Target Name |
Plasminogen
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Gene Name |
PLG
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Synonyms |
Plasmin; PLG
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Target Type |
Successful
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Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
Bleeding [ICD9: 444, 453; ICD10: I74, I80-I82] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63] | |||||
Chronic angina [ICD9: 413; ICD10: I20] | |||||
Excessive bleeding [ICD9: 459; ICD10: R58] | |||||
Excessive postoperative bleeding [ICD9: 459; ICD10: R58] | |||||
Heart attack; Myocardial infarction [ICD9:410; ICD10: I21, I22] | |||||
Ischemic stroke [ICD9: 434.91; ICD10: I61-I63] | |||||
Myocardial infarction; Acute coronary thrombosis [ICD9:410, 414.8; ICD10: I21, I22, I24.0] | |||||
Menorrhagia [ICD9: 627; ICD10: N92.0] | |||||
Macular degeneration [ICD9: 362.5; ICD10: H35.3] | |||||
Myocardial infarction [ICD9: 410; ICD10: I21, I22] | |||||
Otitis media [ICD10: H65-H67] | |||||
Pulmonary embolism [ICD9: 415.1; ICD10: I26] | |||||
Unspecified [ICD code not available] | |||||
Function |
Angiostatin is an angiogenesis inhibitor that blocks neovascularization and growth of experimental primary and metastatic tumors in vivo.
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BioChemical Class |
Peptidase
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Target Validation |
T89034
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UniProt ID | |||||
EC Number |
EC 3.4.21.7
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Sequence |
MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFT
CRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKN GITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILE CEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRE LRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWS AQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTE QLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAG LTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEED CMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGG PWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRT RFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLE PTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQ LPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSW GLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
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Drugs and Mode of Action | |||||
Drug(s) | Alteplase | Drug Info | Approved | Pulmonary embolism | [536186] |
Aminocaproic Acid | Drug Info | Approved | Excessive postoperative bleeding | [538232], [541697] | |
Anistreplase | Drug Info | Approved | Myocardial infarction; Acute coronary thrombosis | [531393], [536361] | |
Ranolazine | Drug Info | Approved | Chronic angina | [528253], [528715], [542312] | |
Ranolazine extended-release | Drug Info | Approved | Unspecified | [551871] | |
Reteplase | Drug Info | Approved | Heart attack; Myocardial infarction | [536361], [551871] | |
Streptokinase | Drug Info | Approved | Pulmonary embolism | [536838] | |
Tenecteplase | Drug Info | Approved | Myocardial infarction | [536523] | |
Tranexamic Acid | Drug Info | Approved | Excessive bleeding | [538522], [541696] | |
Desmoteplase | Drug Info | Phase 3 | Ischemic stroke | [521641] | |
MELAGATRAN | Drug Info | Phase 3 | Discovery agent | [521709], [541520] | |
Plasminogen concentrate | Drug Info | Phase 2/3 | Alzheimer disease | [523835] | |
RetinoStat | Drug Info | Phase 2 | Macular degeneration | [531944] | |
Troplasminogen alfa | Drug Info | Phase 2 | Myocardial infarction | [521672] | |
bis-triazole derivative 10 | Drug Info | Clinical trial | Otitis media | [541664] | |
Inhibitor | 1-(2-Oxo-2-p-tolyl-ethyl)-1H-indole-2,3-dione | Drug Info | [525916] | ||
1-(3,3-Dimethyl-2-oxo-butyl)-1H-indole-2,3-dione | Drug Info | [525916] | |||
1-guanidino-7-isoquinolinesulphonamide | Drug Info | [528796] | |||
1-guanidino-N-phenyl-7-isoquinolinesulphonamide | Drug Info | [528796] | |||
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | [526118] | |||
Aminocaproic Acid | Drug Info | [535448], [535741] | |||
Antifibrinolytic agents | Drug Info | [532368] | |||
Bicine | Drug Info | [551393] | |||
bis-triazole derivative 10 | Drug Info | [531771] | |||
GRASSYSTATIN A | Drug Info | [530345] | |||
MELAGATRAN | Drug Info | [528066] | |||
N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine | Drug Info | [527081] | |||
Textilinin | Drug Info | [532368] | |||
Tranexamic Acid | Drug Info | [536462] | |||
XP-21510 | Drug Info | [532368] | |||
Activator | Alteplase | Drug Info | [536069] | ||
Anistreplase | Drug Info | [537670], [538062] | |||
Desmoteplase | Drug Info | [526538] | |||
M5 | Drug Info | [532368] | |||
Reteplase | Drug Info | [536348], [536795] | |||
Streptokinase | Drug Info | [537005] | |||
Tenecteplase | Drug Info | [536069] | |||
Modulator | Plasminogen concentrate | Drug Info | [527522], [532368] | ||
Ranolazine | Drug Info | [532368] | |||
Ranolazine extended-release | Drug Info | [532368] | |||
RetinoStat | Drug Info | [531944] | |||
SMTP-0 | Drug Info | [532368] | |||
Troplasminogen alfa | Drug Info | [527763], [532368] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Complement and coagulation cascades | |||||
Staphylococcus aureus infection | |||||
Influenza A | |||||
PANTHER Pathway | Blood coagulation | ||||
Plasminogen activating cascade | |||||
Pathway Interaction Database | Angiopoietin receptor Tie2-mediated signaling | ||||
p75(NTR)-mediated signaling | |||||
amb2 Integrin signaling | |||||
Syndecan-4-mediated signaling events | |||||
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
PathWhiz Pathway | Coagulation | ||||
Reactome | Platelet degranulation | ||||
Degradation of the extracellular matrix | |||||
Activation of Matrix Metalloproteinases | |||||
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) | |||||
Dissolution of Fibrin Clot | |||||
WikiPathways | Complement and Coagulation Cascades | ||||
Human Complement System | |||||
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) | |||||
Activation of Matrix Metalloproteinases | |||||
Blood Clotting Cascade | |||||
Dissolution of Fibrin Clot | |||||
Folate Metabolism | |||||
Vitamin B12 Metabolism | |||||
Selenium Micronutrient Network | |||||
References | |||||
Ref 521641 | ClinicalTrials.gov (NCT00111852) Study of Desmoteplase (International Nonproprietary Name [INN]) in Acute Ischemic Stroke (DIAS-2). U.S. National Institutes of Health. | ||||
Ref 521672 | ClinicalTrials.gov (NCT00144014) Safety and Efficacy Study in Acute Ischaemic Stroke. U.S. National Institutes of Health. | ||||
Ref 521709 | ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health. | ||||
Ref 523835 | ClinicalTrials.gov (NCT01554956) Efficacy/Safety of Human Plasminogen Eye Drop in Ligneous Conjunctivitis Patients. U.S. National Institutes of Health. | ||||
Ref 528253 | Late sodium current in the pathophysiology of cardiovascular disease: consequences of sodium-calcium overload. Heart. 2006 Jul;92 Suppl 4:iv1-iv5. | ||||
Ref 531393 | Acylated plasminogen-streptokinase activator complex: a new approach to thrombolytic therapy. Pharmacotherapy. 1990;10(2):115-26. | ||||
Ref 531944 | Safety and biodistribution of an equine infectious anemia virus-based gene therapy, RetinoStat(?), for age-related macular degeneration. Hum Gene Ther. 2012 Sep;23(9):980-91. | ||||
Ref 536186 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536523 | Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. | ||||
Ref 536838 | Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. | ||||
Ref 538232 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071192. | ||||
Ref 538522 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019281. | ||||
Ref 541520 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6382). | ||||
Ref 541664 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6537). | ||||
Ref 541696 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6573). | ||||
Ref 541697 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6574). | ||||
Ref 525916 | Bioorg Med Chem Lett. 2000 Nov 20;10(22):2501-4.Parallel synthesis of isatin-based serine protease inhibitors. | ||||
Ref 526118 | J 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. | ||||
Ref 526538 | Vampire bat salivary plasminogen activator (desmoteplase): a unique fibrinolytic enzyme that does not promote neurodegeneration. Stroke. 2003 Feb;34(2):537-43. | ||||
Ref 527081 | Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. | ||||
Ref 527522 | Structure and function of the plasminogen/plasmin system. Thromb Haemost. 2005 Apr;93(4):647-54. | ||||
Ref 528066 | Bioorg 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. | ||||
Ref 528796 | J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. | ||||
Ref 530345 | J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. | ||||
Ref 531771 | A new strategy for the development of highly potent and selective plasmin inhibitors. J Med Chem. 2012 Feb 9;55(3):1171-80. | ||||
Ref 531944 | Safety and biodistribution of an equine infectious anemia virus-based gene therapy, RetinoStat(?), for age-related macular degeneration. Hum Gene Ther. 2012 Sep;23(9):980-91. | ||||
Ref 532368 | Tranexamic acid in trauma: how should we use it. J Trauma Acute Care Surg. 2013 Jun;74(6):1575-86. | ||||
Ref 535448 | The 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. | ||||
Ref 535741 | 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. | ||||
Ref 536069 | Thrombolytic therapies: the current state of affairs. J Endovasc Ther. 2005 Apr;12(2):224-32. | ||||
Ref 536462 | Evaluation 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. | ||||
Ref 536795 | Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. | ||||
Ref 537005 | Acute 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. |
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