Target Information

Target General Infomation
Target ID
T89034
Former ID
TTDS00392
Target Name
Plasminogen
Gene Name
PLG
Synonyms
Plasmin; PLG
Target Type
Successful
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 [ICD9: 410; ICD10: I21, I22]
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]
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.
BioChemical Class
Peptidase
Target Validation
T89034
UniProt ID
P00747
EC Number
EC 3.4.21.7
Sequence
MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFT
CRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKN
GITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILE
CEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRE
LRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWS
AQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTE
QLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAG
LTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEED
CMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGG
PWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRT
RFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLE
PTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQ
LPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSW
GLGCARPNKPGVYVRVSRFVTWIEGVMRNN
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 521641ClinicalTrials.gov (NCT00111852) Study of Desmoteplase (International Nonproprietary Name [INN]) in Acute Ischemic Stroke (DIAS-2). U.S. National Institutes of Health.
Ref 521672ClinicalTrials.gov (NCT00144014) Safety and Efficacy Study in Acute Ischaemic Stroke. U.S. National Institutes of Health.
Ref 521709ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health.
Ref 523835ClinicalTrials.gov (NCT01554956) Efficacy/Safety of Human Plasminogen Eye Drop in Ligneous Conjunctivitis Patients. U.S. National Institutes of Health.
Ref 528253Late sodium current in the pathophysiology of cardiovascular disease: consequences of sodium-calcium overload. Heart. 2006 Jul;92 Suppl 4:iv1-iv5.
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 531393Acylated plasminogen-streptokinase activator complex: a new approach to thrombolytic therapy. Pharmacotherapy. 1990;10(2):115-26.
Ref 531944Safety 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 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 536361Natural 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 536523Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70.
Ref 536838Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.
Ref 538232FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071192.
Ref 538522FDA 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 542312(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: 7291).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525916Bioorg Med Chem Lett. 2000 Nov 20;10(22):2501-4.Parallel synthesis of isatin-based serine protease inhibitors.
Ref 526118J 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 526538Vampire bat salivary plasminogen activator (desmoteplase): a unique fibrinolytic enzyme that does not promote neurodegeneration. Stroke. 2003 Feb;34(2):537-43.
Ref 527081Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Ref 527522Structure and function of the plasminogen/plasmin system. Thromb Haemost. 2005 Apr;93(4):647-54.
Ref 527763V-10153 (Vernalis). Curr Opin Investig Drugs. 2005 Sep;6(9):951-5.
Ref 528066Bioorg 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 528796J 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 530345J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
Ref 531771A new strategy for the development of highly potent and selective plasmin inhibitors. J Med Chem. 2012 Feb 9;55(3):1171-80.
Ref 531944Safety 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 532368Tranexamic acid in trauma: how should we use it. J Trauma Acute Care Surg. 2013 Jun;74(6):1575-86.
Ref 535448The 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 535741Analysis 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 536069Thrombolytic therapies: the current state of affairs. J Endovasc Ther. 2005 Apr;12(2):224-32.
Ref 536348Spotlight on reteplase in thrombotic occlusive disorders. BioDrugs. 2007;21(1):65-8.
Ref 536462Evaluation 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 536795Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.
Ref 537005Acute 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.
Ref 537670Therapeutic management of acute myocardial infarction. Am J Hosp Pharm. 1990 Sep;47(9 Suppl 2):S5-10.
Ref 538062Evaluation of thrombolytic agents. Drugs. 1997;54 Suppl 3:11-6; discussion 16-7.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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