DT-Web

DB00009 - Alteplase


Identification
Name Alteplase
Accession Number DB00009 (BIOD00050, BTD00050)
Type biotech
Description Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 59042.3000
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication For management of acute myocardial infarction, acute ischemic strok and for lysis of acute pulmonary emboli
Mechanism of action Alteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Nitroglycerin IV nitroglycerin may decrease the effect of alteplase.
Ticlopidine Increased bleeding risk. Monitor for signs of bleeding.
Food Interactions Not Available

Targets


Plasminogen
Name Plasminogen
Gene Name PLG
Pharmacological action yes
Actions activator
References
  • Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. - Pubmed
  • Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. - Pubmed
  • Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.2131
Fibrinogen alpha chain
Name Fibrinogen alpha chain
Gene Name FGA
Pharmacological action yes
Actions Not Available
References
  • Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. - Pubmed
  • Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. - Pubmed
  • Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. - Pubmed
DTHybrid score 0.9732
Urokinase plasminogen activator surface receptor
Name Urokinase plasminogen activator surface receptor
Gene Name PLAUR
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 1.0527
Plasminogen activator inhibitor 1
Name Plasminogen activator inhibitor 1
Gene Name SERPINE1
Pharmacological action unknown
Actions Not Available
References
  • Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. - Pubmed
DTHybrid score 1.0024

Predictions


Id Partner name Gene Name Score
1349 Plasminogen activator inhibitor 2 SERPINB2 0.215
3825 Tetranectin CLEC3B 0.1369
2111 Annexin A2 ANXA2 0.1368
3826 Keratin, type II cytoskeletal 8 KRT8 0.1368
3833 Plasma serine protease inhibitor SERPINA5 0.1217
1516 Calnexin CANX 0.1191
1792 Tissue-type plasminogen activator PLAT 0.1188
3834 Nidogen-1 NID1 0.1098
3831 Low-density lipoprotein receptor-related protein 1 LRP1 0.1097
3830 Calreticulin CALR 0.1079
3011 Suppressor of tumorigenicity protein 14 ST14 0.0939
1193 Proteinase-activated receptor 1 F2R 0.0899
1244 Low-density lipoprotein receptor-related protein 2 LRP2 0.0822
2876 Membrane-bound lytic murein transglycosylase B mltB 0.0726
3133 UDP-galactopyranose mutase glf 0.0725
5099 UDP-galactopyranose mutase glf 0.0725
1812 Kallikrein-1 KLK1 0.0676
2353 Apolipoprotein(a) LPA 0.0654
3812 Fibrinogen beta chain [Contains: Fibrinopeptide B] FGB 0.0581
3813 Fibrinogen gamma chain FGG 0.0581
1974 Oligopeptide transporter, kidney isoform SLC15A2 0.0573
1074 Urokinase-type plasminogen activator PLAU 0.0527
723 Cytosolic phospholipase A2 PLA2G4A 0.05
1278 Pro-epidermal growth factor EGF 0.0487
1525 Heparin-binding growth factor 2 FGF2 0.0385
6231 Pepsin A PGA3 0.0383
6011 Chymotrypsinogen B CTRB1 0.0359
6020 Aldehyde oxidase AOX1 0.0358
3865 Serpin B6 SERPINB6 0.03
1959 Platelet factor 4 PF4 0.03
1986 Ceruloplasmin CP 0.0299
19 Coagulation factor VIII F8 0.026
2021 Thrombomodulin THBD 0.0254
46 Coagulation factor V F5 0.0254
2072 Endothelial protein C receptor PROCR 0.0253
3176 Trypsin-1 PRSS1 0.0248
1245 Vitamin K-dependent protein S PROS1 0.0232
587 Serum albumin ALB 0.0203
448 Vitamin K-dependent gamma-carboxylase GGCX 0.0196
6221 Steroid hormone receptor ERR1 ESRRA 0.0127
1457 Long-chain-fatty-acid--CoA ligase 4 ACSL4 0.0116
54 Prothrombin F2 0.0113
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.01
6177 UDP-glucuronosyltransferase 1-10 UGT1A10 0.01
3809 Estrogen-related receptor gamma ESRRG 0.0097
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.009
2222 Equilibrative nucleoside transporter 1 SLC29A1 0.0088
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0077
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0072
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0072
776 Bile salt export pump ABCB11 0.007
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.007
238 Peroxisome proliferator-activated receptor gamma PPARG 0.0069
3811 Cytochrome P450 19A1 CYP19A1 0.0067
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0063
4878 Glycoprotein hormones alpha chain CGA 0.0062
4877 Beta-mannanase man 0.0062
4869 Major capsid protein A430L 0.0062
4871 Endo-beta-N-acetylglucosaminidase F3 endOF3 0.0062
4850 Beta-2-glycoprotein 1 APOH 0.0062
4880 Membrane cofactor protein CD46 0.0062
1052 Cytotoxic T-lymphocyte protein 4 CTLA4 0.0062
4856 CD209 antigen CD209 0.0062
4889 Ig epsilon chain C region IGHE 0.0062
4189 Alpha-galactosidase A GLA 0.0062
1072 Granzyme B GZMB 0.0062
4852 Reticulon-4 receptor RTN4R 0.0061
757 Fusion glycoprotein F0 F 0.0061
4875 Fusion glycoprotein F0 F 0.0061
4721 Beta-1,4-mannanase manA 0.0061
1563 Platelet glycoprotein Ib alpha chain GP1BA 0.0061
1354 Beta-glucuronidase GUSB 0.0061
442 Envelope glycoprotein gp41 0.0061
4859 Envelope glycoprotein env 0.0061
4845 ADAM 33 ADAM33 0.0061
4882 Dipeptidyl aminopeptidase-like protein 6 DPP6 0.0061
3352 Structural polyprotein Not Available 0.0061
3628 Structural polyprotein Not Available 0.0061
4892 Structural polyprotein Not Available 0.0061
6024 Cytochrome P450 1A1 CYP1A1 0.0058
6107 Cytochrome P450 3A7 CYP3A7 0.0055
6030 Cytochrome P450 2B6 CYP2B6 0.0054
793 T-cell surface antigen CD2 CD2 0.0054
4861 Interleukin-6 receptor alpha chain IL6R 0.0054
119 Carcinoembryonic antigen-related cell adhesion molecule 1 CEACAM1 0.0054
4193 Atrial natriuretic peptide clearance receptor NPR3 0.0054
3837 Cytokine receptor common beta chain CSF2RB 0.0054
1184 Interferon beta IFNB1 0.0052
4857 Zinc-alpha-2-glycoprotein AZGP1 0.0052
6858 Inactive carboxylesterase 4 CES1P1 0.0052
1379 Interleukin-12 subunit beta IL12B 0.0052
554 Low-density lipoprotein receptor LDLR 0.0052
4890 Hemagglutinin HA 0.0052
6566 Hemagglutinin Not Available 0.0052
4118 Cytochrome P450 3A5 CYP3A5 0.0051
4924 Cytochrome P450 2C8 CYP2C8 0.005
6016 Cytochrome P450 2C19 CYP2C19 0.0049
2998 Sialic acid-binding Ig-like lectin 7 SIGLEC7 0.0048
852 Heparin cofactor 2 SERPIND1 0.0048
6120 Cation-independent mannose-6-phosphate receptor IGF2R 0.0048
2297 Genome polyprotein Not Available 0.0048
2322 Genome polyprotein Not Available 0.0048
2694 Genome polyprotein Not Available 0.0048
2719 Genome polyprotein Not Available 0.0048
2860 Genome polyprotein Not Available 0.0048
2928 Genome polyprotein Not Available 0.0048
3160 Genome polyprotein Not Available 0.0048
3260 Genome polyprotein Not Available 0.0048
4783 Genome polyprotein Not Available 0.0048
5726 Genome polyprotein Not Available 0.0048
5779 Genome polyprotein Not Available 0.0048
5867 Genome polyprotein Not Available 0.0048
6253 Genome polyprotein Not Available 0.0048
6301 Genome polyprotein Not Available 0.0048
6380 Genome polyprotein Not Available 0.0048
6381 Genome polyprotein Not Available 0.0048
6437 Genome polyprotein Not Available 0.0048
6520 Genome polyprotein Not Available 0.0048
6521 Genome polyprotein Not Available 0.0048
6652 Genome polyprotein Not Available 0.0048
6734 Genome polyprotein Not Available 0.0048
6735 Genome polyprotein Not Available 0.0048
6736 Genome polyprotein Not Available 0.0048
6737 Genome polyprotein Not Available 0.0048
6738 Genome polyprotein Not Available 0.0048
6739 Genome polyprotein Not Available 0.0048
6744 Genome polyprotein Not Available 0.0048
6748 Genome polyprotein Not Available 0.0048
6894 Genome polyprotein Not Available 0.0048
6898 Genome polyprotein Not Available 0.0048
18 High affinity immunoglobulin epsilon receptor subunit alpha FCER1A 0.0048
3444 Cyanovirin-N Not Available 0.0047
3258 Mannosyl-oligosaccharide alpha-1,2-mannosidase MSDC 0.0047
3140 Hemagglutinin-neuraminidase HN 0.0047
3609 Hemagglutinin-neuraminidase HN 0.0047
1859 Prostatic acid phosphatase ACPP 0.0047
4757 Cytochrome P450 2C9 CYP2C9 0.0046
4787 Envelope glycoprotein gp160 env 0.0045
4820 Envelope glycoprotein gp160 env 0.0045
5727 Envelope glycoprotein gp160 env 0.0045
4666 Fucose-binding lectin PA-IIL lecB 0.0045
2372 Bifunctional tail protein 9 0.0045
2577 Endoplasmic reticulum mannosyl-oligosaccharide 1,2-alpha-mannosidase MAN1B1 0.0042
3480 Mannan endo-1,4-beta-mannosidase manA 0.0041
64 Neuraminidase NA 0.0041
641 Neuraminidase NA 0.0041
2676 Neuraminidase NA 0.0041
3026 Neuraminidase NA 0.0041
3519 Neuraminidase NA 0.0041
6007 Neuraminidase NA 0.0041
4512 Cytochrome P450 3A4 CYP3A4 0.004
1439 Lactotransferrin LTF 0.0039
1782 Neutrophil gelatinase-associated lipocalin LCN2 0.0039
1243 Cathepsin D CTSD 0.0039
958 Insulin-like growth factor 1 receptor IGF1R 0.0039
309 Antithrombin-III SERPINC1 0.0038
2430 Chondroitinase B cslB 0.0037
2581 Chondroitinase AC cslA 0.0037
6847 Lactase-phlorizin hydrolase LCT 0.0037
6307 Ig gamma-2 chain C region IGHG2 0.0037
6500 Phospholipase A2 PLA2G1B 0.0035
2207 Rhodopsin RHO 0.0034
3814 Complement C1r subcomponent C1R 0.0034
4785 Ig gamma-1 chain C region IGHG1 0.003
4604 Liver carboxylesterase 1 CES1 0.003
76 Nitric-oxide synthase, brain NOS1 0.003
952 Dipeptidyl peptidase 4 DPP4 0.0026
3923 Cholinesterase BCHE 0.0025
20 Prostaglandin G/H synthase 1 PTGS1 0.0023
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