Information on EC 3.4.21.68 - t-Plasminogen activator and Organism(s) Homo sapiens and UniProt Accession P00750

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Homo sapiens
UNIPROT: P00750
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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
3.4.21.68
-
RECOMMENDED NAME
GeneOntology No.
t-Plasminogen activator
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
CAS REGISTRY NUMBER
COMMENTARY hide
139639-23-9
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
malfunction
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
D-Ile-Pro-Arg-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
di-Glu-Pro-Arg-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
methylsulfonyl-D-cyclohexylglycyl-Arg-7-amido-4-methylcoumarin + H2O
methylsulfonyl-D-cyclohexylglycyl-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
chromogenic substrate
-
-
?
methylsulfonyl-D-cyclohexyltyrosyl-glycyl-arginine-p-nitroanilide + H2O
methylsulfonyl-D-cyclohexyltyrosyl-glycyl-arginine + p-nitroaniline
show the reaction diagram
-
a chromogenic substrate
-
-
?
N-methyl-D-aspartate receptor + H2O
?
show the reaction diagram
-
usage of total rat brain lysates or MBP-ATD2B fusion proteins, the recombinant human enzyme shows cleavage of the ATD sequence in the NR2B subunit N-terminus of N-methyl-D-aspartate (NMDA) receptor. Enzyme-mediated degradation of NR2B is plasmin-independent. The enzyme cleaves the MBP-ATD2B fusion protein
an Arg27-Arg67-truncated NR2B-containing NMDA receptor might be formed
-
?
plasmin + H2O
?
show the reaction diagram
-
-
-
-
?
plasminogen + H2O
plasmin + ?
show the reaction diagram
thrombin + H2O
?
show the reaction diagram
-
-
-
-
?
(p-F)-FPRANSNH-C2H5 + H2O
(p-F)-FPR + ANSNH-C2H5
show the reaction diagram
-
-
-
?
Asp-Gly-Arg-p-nitroanilide + H2O
Asp-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-Asp(O-tert-butyl)-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-Asp(O-tert-butyl)-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-Asp-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-Asp-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-D-Asp(O-tert-butyl)-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-D-Asp(O-tert-butyl)-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-D-Glu(O-tert-butyl)-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-D-Glu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-D-Glu-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-D-Glu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-D-Phe-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-D-Phe-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-Glu(O-tert-butyl)-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-Glu(O-tert-butyl)-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-pyroglutamic acid-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-pyroglutamic acid-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-Val-Gly-Arg-p-nitroanilide + H2O
benzyloxycarbonyl-Val-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
Boc-(p-F)-FPRANSNH-C2H5 + H2O
Boc-(p-F)-FPR + ANSNH-C2H5
show the reaction diagram
-
-
-
?
Boc-D-FLRANSNH-C3H7 + H2O
Boc-D-FLR + ANSNH-C3H7
show the reaction diagram
-
-
-
?
Boc-D-FPRANSNH-C6H11 + H2O
Boc-D-FPR + ANSNH-C6H11
show the reaction diagram
-
-
-
?
Boc-D-FVRANSNH-C2H5 + H2O
Boc-D-FVR + ANSNH-C2H5
show the reaction diagram
-
-
-
?
Boc-D-LGRANSNH-C6H11 + H2O
Boc-D-LGR + ANSNH-C6H11
show the reaction diagram
-
-
-
?
Boc-D-LPRANSNH-C3H7 + H2O
Boc-D-LPR + ANSNH-C3H7
show the reaction diagram
-
-
-
?
Boc-D-LSRANSNH-C3H7 + H2O
Boc-D-LSR + ANSNH-C3H7
show the reaction diagram
-
-
-
?
Boc-D-VGRANSNH-C4H9 + H2O
Boc-D-VGR + ANSNH-C4H9
show the reaction diagram
-
-
-
?
Boc-D-VPRANSNH-C4H9 + H2O
Boc-D-VPR + ANSNH-C4H9
show the reaction diagram
-
-
-
?
Boc-L-FPRANSNH-C2H5 + H2O
Boc-L-FPR + ANSNH-C2H5
show the reaction diagram
-
-
-
?
Boc-L-VGRANSNH-C4H9 + H2O
Boc-L-VGR + ANSNH-C4H9
show the reaction diagram
-
-
-
?
cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
cyclohexylglycyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-Asp-Gly-Arg-p-nitroanilide + H2O
D-Asp-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
D-cyclohexylglycyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-FLRANSNH-C3H7 + H2O
D-FLR + ANSNH-C3H7
show the reaction diagram
-
-
-
?
D-FPR ANSNH-C6H11 + H2O
D-FPR + ANSNH-C6H11
show the reaction diagram
-
-
-
?
D-FPRANSN-(CH2)6 + H2O
D-FPR + ANSN-(CH2)6
show the reaction diagram
-
-
-
?
D-FPRANSN-C2H5 + H2O
D-FPR + ANSN-C2H5
show the reaction diagram
-
-
-
?
D-FPRANSNH-c-C6H11 + H2O
D-FPR + ANSNH-c-C6H11
show the reaction diagram
-
-
-
?
D-FPRANSNH-C2H4OCH3 + H2O
D-FPR + ANSNH-C2H4OCH3
show the reaction diagram
-
-
-
?
D-FPRANSNH-C6H5CH2 + H2O
D-FPR + ANSNH-C6H5CH2
show the reaction diagram
-
-
-
?
D-FPRANSNH-CH2COOCH3 + H2O
D-FPR + ANSNH-CH2COOCH3
show the reaction diagram
-
-
-
?
D-FPRANSNH-i-C3H7 + H2O
D-FPR + ANSNH-i-C3H7
show the reaction diagram
-
-
-
?
D-FPRANSNH-n-C4H9 + H2O
D-FPR + ANSNH-n-C4H9
show the reaction diagram
-
-
-
?
D-FPRANSNH-n-C6H13 + H2O
D-FPR + ANSN-H-n-C6H13
show the reaction diagram
-
-
-
?
D-FPRANSNH-t-C4H9 + H2O
D-FPR + ANSNH-t-C4H9
show the reaction diagram
-
-
-
?
D-FVRANSNH-C2H5 + H2O
D-FVR + ANSNH-C2H5
show the reaction diagram
-
-
-
?
D-Glu-Gly-Arg-p-nitroanilide + H2O
D-Glu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-Glu-Phe-Lys-p-nitroanilide + H2O
D-Glu-Phe-Lys + p-nitroaniline
show the reaction diagram
-
-
-
-
-
D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide + H2O
D-hexahydrotyrosyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-Ile-Pro-Arg-p-nitroanilide + H2O
D-Ile-Pro-Arg + p-nitroaniline
show the reaction diagram
-
-
-
-
?
D-LGRANSNH-C6H11 + H2O
D-LGR + ANSNH-C6H11
show the reaction diagram
-
-
-
?
D-LPRANSNH-C3H7 + H2O
D-LPR + ANSNH-C3H7
show the reaction diagram
-
-
-
?
D-LSRANSNH-C3H7 + H2O
D-LSR + ANSNH-C3H7
show the reaction diagram
-
-
-
?
D-Lys-Gly-Arg-p-nitroanilide + H2O
D-Lys-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-Phe-Gly-Arg-p-nitroanilide + H2O
D-Phe-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-Val-L-Leu-L-Lys-p-nitroanilide + H2O
D-Val-L-Leu-L-Lys + p-nitroaniline
show the reaction diagram
-
-
-
-
?
D-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroanilide
show the reaction diagram
-
-
-
-
?
D-Val-Leu-Lys-p-nitroanilide + H2O
D-Val-Leu-Lys + p-nitroaniline
show the reaction diagram
-
-
-
-
?
D-VGRANSNH-C4H9 + H2O
D-VGR + ANSNH-C4H9
show the reaction diagram
-
-
-
?
D-VPRANSNH-C4H9 + H2O
D-VPR + ANSNH-C4H9
show the reaction diagram
-
-
-
?
Glu-Gly-Arg-p-nitroanilide + H2O
Glu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
Glu-plasminogen + H2O
plasmin + ?
show the reaction diagram
-
-
-
-
?
glutaryl-Gly-7-Arg-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
L-VGRANSNH-C4H9 + H2O
L-VGR + ANSNH-C4H9
show the reaction diagram
-
-
-
?
Lys-Lys-Cys-Pro-Gly-Arg-Val-Val-Gly-Gly-Cys-Val-Ala-His + H2O
?
show the reaction diagram
-
-
-
-
-
Lys-Lys-Ser-Pro-Gly-Arg-Val-Val-Gly-Gly-Ser-Val-Ala-His + H2O
?
show the reaction diagram
-
-
-
-
-
Lys-plasminogen + H2O
plasmin + ?
show the reaction diagram
-
-
-
?
methyloxycarbonyl-D-cyclohexylalanyl-Gly-Arg-p-nitroanilide + H2O
methyloxycarbonyl-D-cyclohexylglycyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
methyloxycarbonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
methyloxycarbonyl-D-cyclohexylglycyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
methyloxycarbonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide + H2O
methyloxycarbonyl-D-hexahydrotyrosyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
methyloxycarbonyl-D-Leu-Gly-Arg-p-nitroanilide + H2O
methyloxycarbonyl-D-Leu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
methyloxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide + H2O
methyloxycarbonyl-D-Nle-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
methyloxycarbonyl-D-Val-Gly-Arg-p-nitroanilide + H2O
methyloxycarbonyl-D-Nle-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
methylsulfonyl-D-Phe-Gly-Arg-7-amido-4-methylcoumarin + H2O
methylsulfonyl-D-Phe-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide + H2O
methylsulfonyl-D-Phe-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
MMP-9 + H2O
?
show the reaction diagram
-
tPA directly or by activation of MMP-9, can have beneficial effects on recovery after stroke by promoting neurovascular repair through vascular endothelial growth factor
-
-
?
Peptide S-2288 + H2O
?
show the reaction diagram
-
chromogenic substrate
-
-
-
Phe-Gly-Arg-p-nitroanilide + H2O
Phe-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
plasminogen + H2O
?
show the reaction diagram
plasminogen + H2O
plasmin + ?
show the reaction diagram
plasminogen + H2O
plasminon + ?
show the reaction diagram
-
-
-
-
?
Plasminogen-activator-inhibitor 1 + H2O
?
show the reaction diagram
-
PAI-1 may occur in three interconvertible conformations: latent, inhibitor and substrate
-
-
-
SNase PFGRSA + H2O
SNase-PFGR + Ser-Ala
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PFGRSAG + H2O
SNase-PFGR + Ser-Ala-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PGPFGRSAG + H2O
SNase-PGPFGR + Ser-Ala-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PGPFGRSAGG + H2O
SNase-PGPFGR + Ser-Ala-Gly-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PGSGRSAG + H2O
SNase-PGSGR + Ser-Ala-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PHYGRSGG + H2O
SNase-PHYGR + Ser-Gly-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PPFGRSAG + H2O
SNase-PPFGR + Ser-Ala-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
SNase PQRGRSAG + H2O
SNase-PQRGR + Ser-Ala-Gly
show the reaction diagram
-
staphylococcal nuclease with substitutions for amino acids 44-51
-
?
spectrozyme tPA + H2O
?
show the reaction diagram
-
-
-
?
tert-butyloxycarbonyl-Gly-Gly-Arg-p-nitroanilide + H2O
tert-butyloxycarbonyl-Gly-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
Val-Leu-Lys-p-nitroanilide + H2O
p-nitroaniline + ?
show the reaction diagram
-
i.e. S-2251
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
plasminogen + H2O
plasmin + ?
show the reaction diagram
plasminogen + H2O
?
show the reaction diagram
plasminogen + H2O
plasmin + ?
show the reaction diagram
plasminogen + H2O
plasminon + ?
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
native and recombinant beta2-glycoprotein I or its domain V stimulate tPA-dependent plasminogen activation in a concentration-dependent manner. Beta2-glycoprotein I binds tPA with high affinity (Kd =20 nmol), stimulates tPA amidolytic activity, and causes an overall 20fold increase in the catalytic efficiency (kcat/Km) of tPA-mediated conversion of Glu-plasminogen to plasmin
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
-
-
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
-
4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
-
-
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
-
-
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
-
-
6-carbamimidoyl-N-phenyl-2-naphthamide
-
-
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
-
-
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
-
-
6-methoxy-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
-
-
6-methoxy-N-(3'-nitrobiphenyl-4-yl)-2-naphthamide
-
-
alpha2-antiplasmin
-
-
-
Aprotinin
-
-
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
-
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
-
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
-
methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-methoxy-2-naphthamido)biphenyl-3-carboxylate
-
-
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
-
-
N-((2-(iodoacetoxy)ethyl)-N-methyl)amino-7-nitrobenz-2-oxa-3-diazole
-
P9 plasminogen activator inhibitor-1
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
-
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
-
N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
-
plasminogen activator inhibitor 1
-
physiological inhibitor
plasminogen activator inhibitor type 1
-
an important inhibitor of plasminogen activators
-
plasminogen activator inhibitor-1
xenon
-
intraischemic xenon dose-dependently inhibits tissue-type plasminogen activator-induced thrombolysis and subsequent reduction of ischemic brain damage, postischemic xenon virtually suppresses ischemic brain damage and tissue-type plasminogen activator-induced brain hemorrhages and disruption of the blood-brain barrier, therefore xenon should not be administered before or together with a tissue-type plasminogen activator therapy
1,5-Dansyl-L-glutamylglycyl-L-arginine chloromethyl ketone
-
-
2,5-Bis(4-amidinobenzylidene)cyclopentanone
-
-
2,6-Bis(4-amidinobenzylidene)cyclohexanone
-
-
2,7-Bis(4-amidinobenzylidene)cycloheptanone
-
-
2,8-Bis(4-amidinobenzylidene)cyclooctanone
-
-
alpha-1-Proteinase inhibitor
-
-
-
alpha-2-Antiplasmin
-
-
-
alpha-2-Macroglobulin
-
-
-
benzamidine
-
-
C1-inhibitor
-
-
-
Cd2+
-
inhibition of amidolytic activity
Cell/platelet-type plasminogen activator inhibitor
-
from bovine aortic endothelial
-
Co2+
-
inhibition of amidolytic activity
Cu2+
-
inhibition of amidolytic activity
Fast-acting plasminogen activator inhibitor in plasma
-
-
-
Gabexate
-
-
Hg2+
-
inhibition of amidolytic activity
Human plasminogen activator inhibitors
-
leupeptin
-
-
mesilate
-
-
Myxoma virus serine proteinase inhibitor
-
-
-
NaCl
-
high concentrations inhibit the binding of beta2-glycoprotein I to tPA
neuroserpin
-
endogenous inhibitor, regulating tPA activity
-
Ni2+
-
inhibition of amidolytic activity
p-aminobenzamidine
-
-
PAI-1 inhibitor
-
-
-
Placental-type plasminogen activator inhibitor
-
-
-
plasminogen
-
substrate inhibition, at low concentrations of t-PA and D-dimer of fibrin containing the D-domain of fibrin in the presence of physiological concentrations of plasminogen
-
plasminogen activator inhibitor
-
PAI-1
-
plasminogen activator inhibitor type 1
-
pregnant women have higher plasma plasminogen activator inhibitor type 1 antigen concentrations that result in lower basal t-PA/plasminogen activator inhibitor type 1 ratios and plasma t-PA activity concentrations
-
plasminogen activator inhibitor type 1 (PAI-1)
-
-
-
plasminogen activator inhibitor-1
plasminogen activator inhibitor-1 (PAI-1)
-
; sctPA is more susceptible to PAI-1 in buffer solution and in the presence of fibrinogen. In the presence of fibrin there is no difference between single-chain enzyme tPA (sctPA) and two chain tPA (tctPA)
-
plasminogen activator inhibitor-I
-
rapidly inactivates the catalytic activity of tPA in the blood stream
-
propanolol
-
in normotensive subjects, t-PA release by epinephrine is abolished in the presence of propanolol (10 microg/100 ml per minute). In essential hypertensive patients, the response to isoproterenol is impaired as compared with normotensive subjects and is unaffected by NG-monomethyl-L-arginine coinfusion
Protease nexin-like plasminogen activator inhibitor
-
-
-
serpin plasminogen activator inhibitor (PAI)-1
-
primary physiological inhibitor
-
Zn2+
-
inhibition of amidolytic activity
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Fibrin
-
activates the wild-type enzyme, and also the chimeric mutant enzyme, the latter to an extremely higher degree, overview
melanotransferrin
-
-
-
adenosine
-
potentiates mast cell tPA activity and tPA gene expression, abolished in the presence of adenosine deaminase
bradykinin
-
endothelium-dependent vasodilator that stimulates the release of t-PA. Causes a dose-dependent increase in plasma t-PA antigen and activity concentrations in the infused arm of both pregnant and non-pregnant women. The increase in t-PA activity is greater in the nonpregnant women. Bradykinin increases the net release of t-PA antigen and activity in both pregnant women and non-pregnant women. Both net release of active t-PA and plasma t-PA/plasminogen activator inhibitor type 1 ratios are markedly reduced in pregnant women
cyanogen bromide-treated fibrinogen (CNBr-Fbg)
-
CNBr-Fbg (50 microgram/ml) give a 10-fold enhancement of activation, and addition of 2.86 microg/ml oversulfated chondroitin-6-sulfate or oversulfated fucoidan amplified this to 15-fold. A 25-fold to 35-fold enhancement of activation of glutamic plasminogen by tPA is obtained when 2.86 microgram/ml oversulfated compounds are combined with 16.2 mmol/l lysine and 50 microgram/ml CNBr-Fbg
-
epinephrine
-
intrabrachial infusion of epinephrine (0.1 to 0.3 microg/100 ml per minute) induces greater t-PA release in normotensive subjects as compared with essential hypertensive patients
Fibrin
fibrinogen
-
activation induced by
-
isoproterenol
-
intrabrachial isoproterenol (0.03 mcirog/100 ml per minute) induces a significant increase in t-PA release, an effect blunted by NG-monomethyl-L-arginine
L-lysine
-
addition of 16.2 mmol/l L-lysine give 3fold to 4fold enhancement of activation, which is further enhanced to 5fold to 6fold by addition of 2.86 microgram/ml oversulfated chondroitin-6-sulfate or oversulfated fucoidan
oversulfated chondroitin-6-sulfate
-
addition of 28.6 microgram/ml gives 2-fold to 4-fold increase in the rate of enhancement of activation of glutamic plasminogen by tPA using 0.05 mol/l Tris buffer (pH 7.35) containing NaCl (0.9%)
-
oversulfated fucoidan
-
addition of 28.6 microgram/ml gives 2-fold to 4-fold increase in the rate of enhancement of activation of glutamic plasminogen by tPA using 0.05 mol/l Tris buffer (pH 7.35) containing NaCl (0.9%)
-
plasminogen activator inhibitor-1
-
dose-dependently facilitates the dissociation of membrane-retained tPA and increases the amounts of tPA-plasminogen activator inhibitor-1 high-molecular-weight complexes in the medium
Polymerized fibrin
-
enhances amidolytic activity of both one-chain tPA forms but not of two-chain tPA
-
statins
-
can induce tPA and inhibits plasminogen activator inhibitor-1
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0004 - 0.39
(p-F)-FPRANSNH-C2H5
0.86
Asp-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
2.3
benzyloxycarbonyl-Asp(O-tert-butyl)-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.72
benzyloxycarbonyl-Asp-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.52
benzyloxycarbonyl-D-Arg-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
1.8
benzyloxycarbonyl-D-Asp(O-tert-butyl)-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
1.2
benzyloxycarbonyl-D-Glu(O-tetr-butyl)-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
2.6
benzyloxycarbonyl-D-Glu-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.3
benzyloxycarbonyl-D-Phe-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.9
benzyloxycarbonyl-Glu-(O-tert-butyl)Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
2.2
benzyloxycarbonyl-Glu-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
1.36
benzyloxycarbonyl-Val-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.0004 - 0.071
Boc-(p-F)-FPRANSNH-C2H5
0.013 - 0.03
Boc-D-FLRANSNH-C3H7
0.0008
Boc-D-FLRANSNHC3H7
-
pH 7.4, 25°C, ratio tc/sc
0.0026 - 0.047
Boc-D-FPRANSNH-C6H11
0.0027 - 0.091
Boc-D-FVRANSNH-C2H5
0.0004 - 0.023
Boc-D-LGRANSNH-C6H11
0.0006 - 0.066
Boc-D-LPRANSNH-C3H7
0.0006 - 0.36
Boc-D-LSRANSNH-C3H7
0.0007 - 0.14
Boc-D-VGRANSNH-C4H9
0.0005
Boc-D-VPR-ANSNHC4H9
-
pH 7.4, 25°C, ratio tc/sc
0.015 - 0.029
Boc-D-VPRANSNH-C4H9
0.1
Boc-L-VGRANSNHC4H9
-
pH 7.4, 25°C
5.32
cyclohexylglycyl-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
1.7
D-Asp(O-tert-butyl)-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
1.53
D-cyclohexylglycyl-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.0074 - 0.01
D-FLRANSNH-C3H7
0.00078
D-FPR-ANSNH-C2H4OCH3
-
pH 7.4, 25°C, ratio tc/sc
0.00046
D-FPR-ANSNH-CH2COOCH3
-
pH 7.4, 25°C, ratio tc/sc
0.099
D-FPR-ANSNH-n-C6H13
-
pH 7.4, 25°C, sc-tPA
0.00038 - 0.25
D-FPRANSN-(CH2)6
0.00037 - 0.32
D-FPRANSN-C2H5-C2H5
0.00059 - 0.15
D-FPRANSNH-c-C6H11
0.14 - 0.18
D-FPRANSNH-C2H4OCH3
0.0057 - 0.077
D-FPRANSNH-C6H11
0.0004 - 0.063
D-FPRANSNH-C6H5CH2
0.029 - 0.063
D-FPRANSNH-CH2COOCH3
0.00022 - 0.33
D-FPRANSNH-i-C3H7
0.0004 - 0.12
D-FPRANSNH-n-C4H9
0.095 - 0.096
D-FPRANSNH-n-C6H13
0.0011 - 0.084
D-FPRANSNH-t-C4H9
0.0011 - 0.016
D-FVRANSNH-C2H5
2.9
D-Glu-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.83
D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.000086 - 0.694
D-Ile-Pro-Arg-p-nitroanilide
0.001 - 0.041
D-LGRANSNH-C6H11
0.0003 - 0.098
D-LPRANSNH-C3H7
0.0012 - 0.069
D-LSRANSNH-C3H7
2.1
D-Lys-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.7
D-Phe-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.0015 - 0.058
D-VGRANSNH-C4H9
0.0003 - 0.11
D-VPRANSNH-C4H9
3.2
Glu-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.00002 - 0.065
Glu-plasminogen
-
0.036 - 0.97
L-FPRANSNH-C2H5
0.46
L-VGRANSNH-C4H9
-
pH 7.4, 25°C
5.9
Lys-Lys-Cys-Pro-Gly-Arg-Val-Val-Gly-Gly-Cys-Val-Ala-His
-
-
3.6
Lys-Lys-Ser-Pro-Gly-Arg-Val-Val-Gly-Gly-Ser-Val-Ala-His
-
-
0.00001 - 0.019
Lys-plasminogen
-
0.34
methyloxycarbonyl-D-cyclohexylalanyl-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.42
methyloxycarbonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.39
methyloxycarbonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.62
methyloxycarbonyl-D-Leu-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.99
methyloxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.8
methyloxycarbonyl-D-Val-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.1
methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.000017
Peptide S-2288
-
-
3.15
pGlu-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
2
Phe-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
0.000018 - 0.065
plasminogen
-
0.14
SNase PFGRSA
-
pH 7.4, 37°C
-
0.079
SNase PFGRSAG
-
pH 7.4, 37°C
-
0.0099
SNase PGPFGRSAG
-
pH 7.4, 37°C
-
0.0093
SNase PGPFGRSAGG
-
pH 7.4, 37°C
-
0.017
SNase PGSGRSAG
-
pH 7.4, 37°C
-
0.018
SNase PHYGRSGG
-
pH 7.4, 37°C
-
0.0099
SNase PPFGRSAG
-
pH 7.4, 37°C
-
0.0089
SNase PQRGRSAG
-
pH 7.4, 37°C
-
0.4 - 4.6
spectrozyme tPA
3.5
tert-butoxycarbonyl-Gly-Gly-Arg-p-nitroanilide
-
pH 8.0, 25°C
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.099 - 6.08
(p-F)-FPRANSNH-C2H5
0.11 - 6.08
Boc-(p-F)-FPRANSNH-C2H5
0.01 - 4.7
Boc-D-FLRANSNH-C3H7
0.017 - 0.15
Boc-D-FPRANSNH-C6H11
7.9
Boc-D-FVR-ANSNH-C2H5
Homo sapiens
-
pH 7.4, 25°C, ratio tc/sc
0.019 - 0.49
Boc-D-FVRANSNH-C2H5
0.012 - 3.3
Boc-D-LGRANSNH-C6H11
0.038 - 6.08
Boc-D-LPRANSNH-C3H7
0.022 - 6.08
Boc-D-LSRANSNH-C3H7
0.036 - 5
Boc-D-VGRANSNH-C4H9
0.065 - 3.8
Boc-D-VPRANSNH-C4H9
0.084
Boc-L-VGRANSNHC4H9
Homo sapiens
-
pH 7.4, 25°C
0.018
D-FLRANSNH-C3H7
Homo sapiens
-
pH 7.4, 25°C, tc-tPA
0.016
D-FPR-ANSNH-C6H11
Homo sapiens
-
pH 7.4, 25°C, sc-tPA
0.45
D-FPR-ANSNH-C6H5CH2
Homo sapiens
-
pH 7.4, 25°C, sc-tPA
0.47
D-FPR-ANSNH-n-C4H9
Homo sapiens
-
pH 7.4, 25°C, tc-tPA
3.3 - 3.6
D-FPR-ANSNH-n-C6H13
3.8
D-FPR-ANSNH-t-C4H9
Homo sapiens
-
pH 7.4, 25°C, ratio tc/sc
0.51 - 6.08
D-FPR-ANSNHC6H11
0.13 - 1.7
D-FPRANSN-(CH2)6
0.09 - 1.6
D-FPRANSN-C2H5-C2H5
0.15
D-FPRANSN-H-c-C6H11
Homo sapiens
-
pH 7.4, 25°C, sc-tPA
0.2
D-FPRANSN-H-i-C3H7
Homo sapiens
-
pH 7.4, 25°C, tc-tPA
0.25 - 6.08
D-FPRANSN-H-t-C4H9
0.32 - 2.1
D-FPRANSNH-c-C6H11
0.27 - 6.08
D-FPRANSNH-C2H4OCH3
32
D-FPRANSNH-C6H11
Homo sapiens
-
pH 7.4, 25°C, ratio tc/sc
0.54 - 6.08
D-FPRANSNH-C6H5CH2
0.083 - 1.8
D-FPRANSNH-CH2COOCH3
0.29 - 6.08
D-FPRANSNH-i-C3H7
0.33 - 1.4
D-FPRANSNH-n-C4H9
1.1
D-FPRANSNH-n-C6H13
Homo sapiens
-
pH 7.4, 25°C, sc-tPA
0.025
D-FVR-ANSNH-C2H5
Homo sapiens
-
pH 7.4, 25°C, tc-tPA
0.011 - 2.3
D-FVRANSNH-C2H5
0.026 - 10.7
D-Ile-Pro-Arg-p-nitroanilide
0.034 - 4
D-LGR-ANSNH-C6H11
0.0084 - 0.057
D-LGRANSNH-C6H11
0.061 - 2.8
D-LPRANSNH-C3H7
0.019 - 5.3
D-LSRANSNH-C3H7
89
D-LSRANSNHC3H7
Homo sapiens
-
pH 7.4, 25°C
0.021 - 9
D-VGRANSNH-C4H9
0.059 - 2.7
D-VPRANSNH-C4H9
0.04
L-FPRANSNH-C2H5
Homo sapiens
-
pH 7.4, 25°C
0.08
L-VGRANSNH-C4H9
Homo sapiens
-
pH 7.4, 25°C
0.009
Lys-Lys-Cys-Pro-Gly-Arg-Val-Val-Gly-Gly-Cys-Val-Ala-His
Homo sapiens
-
-
0.0012
Lys-Lys-Ser-Pro-Gly-Arg-Val-Val-Gly-Gly-Ser-Val-Ala-His
Homo sapiens
-
-
0.0005 - 0.21
Lys-plasminogen
-
0.06 - 0.4718
plasminogen
-
0.0041
SNase PFGRSA
Homo sapiens
-
pH 7.4, 37°C
-
0.018
SNase PFGRSAG
Homo sapiens
-
pH 7.4, 37°C
-
0.0075
SNase PGPFGRSAG
Homo sapiens
-
pH 7.4, 37°C
-
0.01
SNase PGPFGRSAGG
Homo sapiens
-
pH 7.4, 37°C
-
0.012
SNase PHYGRSGG
Homo sapiens
-
pH 7.4, 37°C
-
0.011
SNase PPFGRSAG
Homo sapiens
-
pH 7.4, 37°C
-
0.006
SNase PQRGRSAG
Homo sapiens
-
pH 7.4, 37°C
-
2 - 60
spectrozyme tPA
additional information
additional information
Homo sapiens
-
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0318
6-carbamimidoyl-N-phenyl-2-naphthamide
-
pH 7.4-8.3, 37°C
0.0049
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
pH 7.4-8.3, 37°C
0.0584
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
pH 7.4-8.3, 37°C
0.0074
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
pH 7.4-8.3, 37°C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0039
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
Homo sapiens
-
pH 7.4-8.3, 37°C
0.022
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
-
pH 7.4-8.3, 37°C
0.03
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0036
4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.1
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.062
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.125
6-carbamimidoyl-N-phenyl-2-naphthamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0053
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.013
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.021
6-methoxy-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0086
6-methoxy-N-(3'-nitrobiphenyl-4-yl)-2-naphthamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0061
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
Homo sapiens
-
pH 7.4-8.3, 37°C
0.023
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
Homo sapiens
-
pH 7.4-8.3, 37°C
0.011
methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0084
methyl 4'-(6-methoxy-2-naphthamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 7.4-8.3, 37°C
0.026
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
Homo sapiens
-
pH 7.4-8.3, 37°C
0.062
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0097
N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0034
N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 7.4-8.3, 37°C
0.0057
N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
Homo sapiens
-
pH 7.4-8.3, 37°C
additional information
xenon
Homo sapiens
-
although xenon at 25% (v/v) has no effect, xenon at higher concentrations of 37.5, 50 and 75% inhibit the catalytic efficiencies of human enzyme, IC50 is 34.85% (v/v)
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.297
-
-
7.4
-
purified recombinant truncated enzyme, pH 8.3, 37°C
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4 - 8.3
-
assay at, dependent on the substrate
7.4
-
assay at
7.5
-
assay at
7.4
-
assay at
7.8
-
assay at
8.3
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7 - 10
-
7: about 85% of activity maximum, 10: about 80% of activity maximum
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
incubated with culture medium containing polyriboinosinic:polyribocytidylic acid RNA in different concentrations
Manually annotated by BRENDA team
-
transformed, carcinoma
Manually annotated by BRENDA team
-
tPA is expressed widely in the central nervous system and is involved in mechanisms of synaptic regulation and synaptic plasticity, both during development and in the mature brain
Manually annotated by BRENDA team
-
vascular endothelial cell line producing GFP-tagged tPA
Manually annotated by BRENDA team
-
arterial and venous concentrations of t-PA are significantly lower in hypertensive patients than in normotensive subjects
Manually annotated by BRENDA team
-
embryonic lung diploid cells, IMR-90 cells, ATCC, CCL186
Manually annotated by BRENDA team
-
transformed cell line
Manually annotated by BRENDA team
-
transformed
Manually annotated by BRENDA team
-
Bowes melanoma
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
from lung
Manually annotated by BRENDA team
-
of transgenic goat
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
exocytosed tPA-GFP is retained at the membrane surface without retrieval for more than 5 min in a vascular endothelial cell-specific manner. FnEK1K2 domains are responsible for binding of tPA-GFP to the membrane surface
Manually annotated by BRENDA team
additional information
-
colocalised with annexin II
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
19950
-
monomer, kringle domain of tissue-type plasminogen activator, calculated from amino acid sequence
21590
-
monomer, kringle domain of tissue-type plasminogen activator, glycosylated, MALDI analysis
23940
-
monomer, kringle domain of tissue-type plasminogen activator, glycosylated, MALDI analysis
32000
-
single-chain tPA, monomer, SDS-PAGE
63500
-
x * 63500, SDS-PAGE
65000
-
two-chain tPA, monomer, SDS-PAGE
68000
-
x * 68000, recombinant enzyme, SDS-PAGE
70000
-
x * 75000, recombinant chimeric enzyme mutant, SDS-PAGE, x * 70000, wild-type t-PA, SDS-PAGE, the wild-type enzyme holds five domains including finger, epidermal growth factor, kringle 1, kringle 2 and protease
75000
-
x * 75000, recombinant chimeric enzyme mutant, SDS-PAGE, x * 70000, wild-type t-PA, SDS-PAGE, the wild-type enzyme holds five domains including finger, epidermal growth factor, kringle 1, kringle 2 and protease
9553
-
MALDI-TOF-DE-MS
9556
-
calculated from amino acid sequence
28126
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1 * 30882 + 1 * 28126, human, calculation from amino acid sequence
30882
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1 * 30882 + 1 * 28126, human, calculation from amino acid sequence
39590
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human, recombinant domain-deletion mutant BM 06.022, calculation from amino acid sequence
53000
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x * 63000, full-length t-PA, SDS-PAGE, x * 53000, truncated 650 bp t-PA, SDS-PAGE
59010
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human, calculation from amino acid sequence
63000
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x * 63000, full-length t-PA, SDS-PAGE, x * 53000, truncated 650 bp t-PA, SDS-PAGE
65000
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human, sedimentation equilibrium, one-chain form
68000
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natively glycosylated tPA
69000 - 72000
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human, gel filtration
70000
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x * 70000, human, SDS-PAGE
72000
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x * 72000, wild-type enzyme
147000
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by Western blot analysis or by anti-GFP antibody, tPA-GFP-plasminogen activator inhibitor-1 complex
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
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1 * 64000-68000, human, SDS-PAGE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
2.3 A crystal structure
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bis-benzamidine-tPA complex, spacegroup C2, cell constants a : 151.83 A, b : 60.50 A, c =:62.61 A
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crystal structure of many components, crystallizing of full-length intact human t-PA have failed so far
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crystal structure of the kringle 2 domain
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.8
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reversible acid/base unfolding below
29586
5 - 10
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stable
29594
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
95
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5 min, stable
additional information
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-80°C
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Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
glycosylation variant of human tPA
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one-step purification using affinity chromatography with a special monoclonal antibody
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recombinant active full-length and active truncated 650 bp enzymes from Nicotiana tabacum by lysine affinity chromatography and gel filtration
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recombinant enzyme
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recombinant His-tagged kringle 2 plus serine protease domains, K2S, of human tissue plasminogen activator from Escherichia coli by nickel affinity chromatography after cleavage with factor Xa
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recombinant His-tagged truncated enzyme from Leishmania tarentolae by nickel affinity chromatography
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using a lysine-sepharose column.Two chain tPA is generated from wild-type tPA by incubation with plasmin-sepharose
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wild type and recombinant enzyme
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli and Saccharomyces cerevisiae
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recobinant expression of wild-type and mutant enzymes in Pichia pastoris strain GS115, cloning in Escherichia coli strain Top10F
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recombinant expression of the chimeric truncated mutant enzyme using the CHO ATCC CRL9606 expression system, and as soluble His-tagged enzyme in Escherichia coli BL21(DE3) strain with F- dcm ompT hsdS (rB- mB-) gal genotype, comparison of protein potency in batch and fed-batch processes of the two methods, overview
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recombinant overexpression of the enzyme in CHO ATCC CRL-9606 cells and secretion to the cell culture medium, co-expression with CERT S132A, a mutant form of CERT that is resistant to phosphorylation, and XBP1s, method optimization and evaluation, overview. Overexpression of CERT S132A increases the specific productivity of t-PA-producing CHO cells up to 35%, while the heterologous expression of XBP1s does not affect the t-PA expression rate
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a truncated version of tPA is fused to the N terminus of the phasin protein with a thrombin cleavage site as the linker, and then expressed in Escherichia coli strain XL1-Blue on the surface of polyhydroxybutyrate granules using phasin as the affinity tag. Untreate enzyme is expressed in inactive inclusion bodies in the bacteria. The in vivo surface display strategy for functional rPA expression in Escherichia coli is distinct for its efficient folding and easier purification, method optimization, overview. Subcloning in Escherichia coli strain DH5alpha
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cDNA expressed in Escherichia coli in the form of inclusion body
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construction of an oviduct-specific vector containing tissue plasminogen activator protein and green fluorescent protein (pL-2.8OVtPAGFP), and expression in vitro and in vivo in hen eggs, and in oviduct epithelial and 3T3 cells, compared to control vector pEGP-N1. The oviduct-specific vector pL-2.8OVtPAGFP is expressed only in oviduct epithelial cells, no detection in heart, muscle, liver and intestine, whereas pEGP-N1 is detected in oviduct epithelial and 3T3 cells. tPA expressed in egg white and oviduct epithelial cells shows fibrinolytic activity. Subcloning in Escherichia coli
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evaluation of expression methods, overview. Recombinant expression of active full-length and active truncated 650 bp enzymes in Nicotiana tabacum
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expressed in SF9 cells using the Bac-to-Bac baculovirus system
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expression in Escherichia coli
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expression in Escherichia coli; recombinant kringle 1 domain from tissue-type plasminogen activator
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functional expression under transcriptional control of single and multiple rooting loci promoter rolD promoters in hairy roots of Cucumis melon, the t-PA gene is integrated in the genome of hairy roots using Agrobacterium-mediated transformation of melon cotyledons. Highest levels of the recombinant t-PA accumulation in transgenic hairy roots carrying the t-PA transgene occur under the control of single and dual rolD promoters compared to triple and quadruple rolD promoters, method evaluation and optimization, overview; t-PA and synthetic t-PA genes, expression as active enzyme in Curcumis melo cv. Geumssaragi-euncheon hairy roots using Agrobacterium rhizogenes transfection, insertion of the t-PA genes in genomic DNA of transgenic hairy roots. Selection of optimum media for the mass-production of transgenic hairy root and fibrinolytic activity of cultured transgenic hairy roots using the bioreactor
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gene K2S, expression of a His-tagged truncated enzyme form in Leishmania tarentolae using an expression cassette containing kringle 2 and serine protease domains, tissue plasminogen activator, together with a signal sequence derived from Leishmania tarentolae and two fragments of the small subunit ribosomal RNA locus. The recombinant enzyme is functional and secreted to the cell culture medium. Replacement of the human signal sequence tPA with the signal sequence derived from Leishmania increases the secretion of recombinant protein up to 30times
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high-level expression of the kringle 2 plus serine protease domains, K2S, of human tissue plasminogen activator in Escherichia coli strain BL21 as active fusion protein, in which the His-tagged K2S domains are fused to the disulfide isomerase DsbC from Escherichia coli, the recombinant fusion protein is soluble. The active K2S domains are liberated by cleavage through factor Xa. Subcloning in Escherichia coli strain DH5alpha
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hybridoma cell lines expressing Mabs 364, 623, 663, and 700, all directed to wtr-K2 tPA, cDNA cloning, recombinant kringle 2 domain r-K2 tPA expressed in Pichia pastoris cells
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hybridoma cell lines expressing Mabs expression of wild-type and mutant enzyme cDNA by transient transfection of COS cells
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recombinant expression and large-scale production of biochemically active wild-type human enzyme and os a synthetic enzyme in hairy roots of Cucumis melo cv. Geumssaragi-euncheon using binary vector p221 and Agrobacterium rhizogenes strain K599-mediated transformation of cotyledons, method evaluation, overview. WPM medium is found to be more suitable for rapid growth of hairy roots among all the seven media types tested, total yield of hairy roots grown on WPM medium is 621.8 g/L at pH 7.0
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recombinant expression of active and soluble enzyme in leaves of Nicotiana tabacum cv. Xathi under the control of CaMV35S promoter and NOS terminator and with high-expression Kozak sequence and KDEL signal for endoplasmic reticulum retention linked to N- and C-termini of t-PA gene, respectively, using the Agrobacterium tumefaciens transfection method
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recombinant tPA from Genentech, 80% sc-tPA, 20% tc-tPA
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rt-PA is produced by recombinant DNA technology in Chinese hamster ovary cell lines
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subcloned into NheI/BamHI sites in GFP3.1
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the gene encoding full-length human t-PA is cloned into pPICZalphaA expression vector downstream of alcohol oxidase promoter and alpha-mating signal sequence from Saccharomyces cerevisiae and flush with the kex2 cleavage site to express the protein with a native N-terminus. Pichia pastoris strain GS115 is transformed with this cassette, and methanol utilizing (mut+) transformants are selected for production and secretion of functional human t-PA into culture media. Subcloning in Escherichia coli strain Top10 F'
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
basal expression of tissue plasminogen activator is not affected by any of the proinflammatory cytokines TNF-alpha, IL-1beta and IFN-gamma individually or in combination, no increase in tissue plasminogen activator synthesis is observed by ELISA when cells are stimulated with viral polyriboinosinic:polyribocytidylic acid RNA for 3 and 6 h, both with and without cytokine pretreatment
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viral polyriboinosinic:polyribocytidylic acid RNA in the culture medium increases mesangial tissue plasminogen activator expression, exposure of mesangial cells to viral polyriboinosinic:polyribocytidylic acid RNA at a concentration of 0.5 or 5 microg/ml increases significantly tissue plasminogen activator mRNA levels in a dose-dependent manner, an effect which is further enhanced with pretreatment of mesangial cells with the cytokine combination, a significant increase in tissue plasminogen activator protein is observed only when cells are pretreated with the combination of proinflammatory cytokines and additionally stimulated with viral polyriboinosinic:polyribocytidylic acid RNA, after 12 and 24 h of polyriboinosinic:polyribocytidylic acid RNA stimulation, tissue plasminogen activator release increases significantly under basal conditions, an effect which is further enhanced when cells are pretreated with the cytokine combination, the maximum increase is observed at 24 h
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adenosine potentiates mast cell tPA activity and tPA gene expression, abolished in the presence of adenosine deaminase. Adenosine upregulates A2A receptor subtype transcript-expression level in HMC-1 cells and human lung mast cells
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after 6-h exposure to cigarette smoke extract, the expression levels of t-PA protein in 10% and 20% cigarette smoke extract-treated groups reduce significantly when compared with that of control group
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after stimulation with 5% cigarette smoke extract for 0, 4, 6, 8, 12, 24 hours, no significant difference is found at the levels of tissue plasminogen protein and mRNA after 2-h simvastatin pre-treatment
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tPA is induced in epilepsy by a mechanism underlying seizure activity. Expression and cellular distribution of tPA in several epileptogenic pathologies, including hippocampal sclerosis, and developmental glioneuronal lesions, such as focal cortical dysplasia, cortical tubers in patients with the tuberous sclerosis complex and in gangliogliomas, using immuno-cytochemical, western blot and real-time quantitative PCR analysis, overview
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K213A/H214A/R215A/R216A
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construction of a chimeric tissue plasminogen activator (t-PA) through kringle 2 domain removal and replacement of t-PA finger domain with the Vampire bat plasminogen activator one. Vampire bat plasminogen activator (b-PA) is a plasminogen activator with higher fibrin affinity and specificity in comparison to t-PA resulting in reduced probability of hemorrhage. b-PA is also resistant to plasminogen activator inhibitor-1 showing higher half-life compared to other variants of t-PA. The KHRR sequence at the initial part of protease domain is replaced by four alanine residues. The activity of therecombinant protein in the presence of fibrin is 1560 times more than its activity in the absence of fibrin, showing its higher specificity to fibrin. The chimeric enzyme shows 1.2fold higher fibrin binding in comparison to full-length enzyme
F423A
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two chain form, site-directed mutagenesis
F423A/R275E
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single-chain form, site-directed mutagenesis
F423E
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two chain form, site-directed mutagenesis
F423E/R275E
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single-chain form, site-directed mutagenesis
L420A
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two chain form, site-directed mutagenesis
L420A/R275E
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single-chain form, site-directed mutagenesis
L420E
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two chain form, site-directed mutagenesis
L420E/R275E
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single-chain form, site-directed mutagenesis
P422A
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two chain form, site-directed mutagenesis
P422A/R275E
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single-chain form, site-directed mutagenesis
P422E/R275E
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single-chain form, site-directed mutagenesis
P422G/R275E
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single-chain form, site-directed mutagenesis
R275E
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single-chain form, site-directed mutagenesis
R275E/P422E
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site-directed mutagenesis
R275E/P422G
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site-directed mutagenesis
S421E
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two chain form, site-directed mutagenesis
S421E/R275E
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single-chain form, site-directed mutagenesis
S421G
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two chain form, site-directed mutagenesis
S421G/R275E
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single-chain form, site-directed mutagenesis
S478A
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efficacy of expression of the mutant and wild-type is similar, but the mutant does not appear in the culture medium after 24 h either complexed with plasminogen activator inhibitor-1 or in the free form. Intracellular distribution is indistinguishable to the wild-type, but it is present at higher concentrations than the wild-type near the plasma membrane
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
medicine
additional information
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tPA can act as a cytokine, executing its cytoprotective actions via activation of a survival signaling hierarchy in interstitial fibroblasts