3.4.17.20: Carboxypeptidase U
This is an abbreviated version!
For detailed information about Carboxypeptidase U, go to the full flat file.
Word Map on EC 3.4.17.20
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3.4.17.20
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plasminogen
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coagulation
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clot
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fibrinolytic
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thrombosis
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thrombomodulin
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plasmin
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fibrinogen
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pai-1
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bleeding
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inhibitor-1
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antifibrinolytic
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hemostatic
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prothrombin
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zymogen
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venous
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anticoagulant
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thromboembolism
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tissue-type
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d-dimers
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hypofibrinolysis
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profibrinolytic
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thrombolytic
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thrombin-thrombomodulin
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hypercoagulable
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procoagulant
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c5a
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antithrombin
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thrombus
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prothrombotic
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thrombin-antithrombin
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thrombin-mediated
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coagulopathy
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plasmin-antiplasmin
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haemostasis
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thromboplastin
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medicine
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antiplasmin
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alpha2-antiplasmin
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fxiii
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metallocarboxypeptidase
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anaphylatoxins
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molecular biology
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pharmacology
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plasmin-mediated
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thrombophilia
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thrombelastography
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activator-induced
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thrombin-dependent
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rfviia
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t-pa-induced
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thrombin-cleaved
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euglobulin
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diagnostics
- 3.4.17.20
- plasminogen
- coagulation
- clot
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fibrinolytic
- thrombosis
- thrombomodulin
- plasmin
- fibrinogen
- pai-1
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bleeding
- inhibitor-1
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antifibrinolytic
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hemostatic
- prothrombin
- zymogen
- venous
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anticoagulant
- thromboembolism
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tissue-type
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d-dimers
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hypofibrinolysis
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profibrinolytic
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thrombolytic
- thrombin-thrombomodulin
-
hypercoagulable
-
procoagulant
- c5a
- antithrombin
- thrombus
-
prothrombotic
-
thrombin-antithrombin
-
thrombin-mediated
- coagulopathy
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plasmin-antiplasmin
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haemostasis
- thromboplastin
- medicine
- antiplasmin
- alpha2-antiplasmin
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fxiii
- metallocarboxypeptidase
- anaphylatoxins
- molecular biology
- pharmacology
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plasmin-mediated
- thrombophilia
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thrombelastography
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activator-induced
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thrombin-dependent
- rfviia
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t-pa-induced
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thrombin-cleaved
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euglobulin
- diagnostics
Reaction
release of C-terminal Arg and Lys from a polypeptide =
Synonyms
aCAP, activated thrombin activable fibrinolysis inhibitor, activated thrombin-activable fibrinolysis inhibitor, activated thrombin-activatable fibrinolysis inhibitor, active carboxypeptidase B, active thrombin-activatable fibrinolysis inhibitor, Arginine carboxypeptidase, Carboxypeptidase B, pro-, carboxypeptidase B2, Carboxypeptidase R, carboxypeptidase U, Carboxypeptidase-U, CPB2, CPR, CPU, Plasma carboxypeptidase B, plasma carboxypeptidase U, plasma CPB, plasma procarboxypeptidase B, plasma procarboxypeptidase B-like proenzyme, plasma procarboxypeptidase U, pro-pCPB, Procarboxypeptidase B, procarboxypeptidase R, procarboxypeptidase U, proCPU, pTAFI, rTAFI, TAFI, TAFIa, TFAI, thrombin activable fibrinolysis inhibitor, thrombin activatable fibrinolysis inhibitor, Thrombin-activable fibrinolysis inhibitor, thrombin-activatable fibrinolysis inhibitor
ECTree
3.4.17.20 Carboxypeptidase UAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.4.17.20 - Carboxypeptidase U
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(R)-3-(2-aminoethylthio)-2-(3-((R)-3-cyclohexyl-1-oxo-1-((1R,2R,4R)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-ylamino)propan-2-yl)ureido)propanoic acid
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2-(2-amino-pyridin-4-ylmethyl)-3-mercapto-propionic acid
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reversible inhibition, IC50: 0.0032 mM
2-(6-amino-pyridin-3-ylmethyl)-2-mercaptomethyl-butyric acid
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reversible inhibition, IC50: 0.25 mM
2-mercaptomethyl-3-(6-amino-pyridin-3-yl)-2-fluoro-propionic acid
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reversible inhibition, IC50: 0.0005 mM
2-mercaptomethyl-3-(6-amino-pyridin-3-yl)-2-hydroxy-propionic acid
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reversible inhibition, IC50: 0.0009 mM
2-mercaptomethyl-3-piperidin-4-yl-propionic acid
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reversible inhibition, IC50: 0.0032 mM
2-mercaptomethyl-3-pyrrolidin-3-yl-propionic acid
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reversible inhibition, IC50: 0.0016 mM
2-[[(2-carbamimidamidoethyl)sulfanyl]methyl]butanedioic acid
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reversible inhibition, IC50: 0.27 mM
3-(2-amino-thiazol-5-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.0013 mM
3-(6-amino-2-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.0063 mM
3-(6-amino-4-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.0079 mM
3-(6-amino-5-chloro-pyridin-3-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.010 mM
3-(6-amino-5-hydroxymethyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.013 mM
3-(6-amino-5-methyl-pyridin-3-yl)-2-(hydroxymethyl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.083 mM
3-(6-amino-5-methyl-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid
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reversible inhibition, IC50: 0.0016 mM; reversible inhibition, IC50: 0.001 mM
3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid
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reversible inhibition, IC50: 0.0006 mM
3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.0002 mM
3-(6-aminopyridin-3-yl)-2-(1-((5-(5-chlorothiophen-2-yl)isoxazol-3-yl)methyl)-1H-imidazol-4-yl)propanoic acid
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3-(6-aminopyridin-3-yl)-2-[1-(3-methylbutyl)-1H-imidazol-4-yl]propanoic acid
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3-(cis-4-amino-cyclopent-2-yl)-2-mercaptomethyl-propionic acid
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reversible inhibition, IC50: 0.001 mM
3-[(2-carbamimidamidoethyl)sulfanyl]-2-(sulfanylmethyl)propanoic acid
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reversible inhibition, IC50: 0.02 mM
BX-528
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i.e. (S)-2-[3-(aminomethyl)phenyl]-3-hydroxy[(R)-2-methyl-1-[(3-phenylpropyl)sulfonyl]aminopropyl]phosphoryl propanoic acid
DL-mercaptomethyl-3-guanidinoethylthiopropanoic acid
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i.e. Plummer's inhibitor, IC50: 0.029 mM
EF-6265
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i.e. (2S)-7-amino-2-((hydroxyl((R)-2-methyl-1-(3-phenylpropanamido)propyl)phosphoryl)methyl)heptanoic acid
guanidinyl-L-cysteine
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IC50: 0.0094 mM in inhibition of plasma fibrin clot lysis
potato tuber carboxypeptidase inhibitor
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competitive inhibition in the nanomolar range
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[(S)-7-amino-2-[[[(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl]methyl]heptanoic acid]
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IC50: 8.3 nM, potent and highly selective inhibitor. Systemically administered inhibitor enhances fibrinolysis in a dose- and time-dependent manner
EF6265
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i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.00000826 mM, inhibitory effect in vivo, overview
EF6265
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i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.000001 mM
EF6265
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i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.00000389 mM, inhibitory effect in vivo, overview
EF6265
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specific inhibitor of activated form of TAFIa. A pharmacologic study to assess the effect of EF6265 on rat sepsis-induced organ dysfunction models is performed. In the endotoxemia model, posttreatment with EF6265 reduces fibrin deposits in the kidney and liver accompanied by no significant changes in platelet count and fibrinogen concentration in plasma. EF6265 also significantly decreases levels of plasma lactate dehydrogenase and aspartate aminotransferase, markers of organ dysfunction. In the sepsis model, EF6265, simultaneously administered with ceftazidime (CAZ) 2 h after Pseudomonas aeruginosa injection dramatically potentiates the interleukin-6-reducing effect of CAZ in plasma. This combined treatment also lowers plasma lactate dehydrogenase and blood urea nitrogen more potently than single treatment with CAZ
MERGETPA
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D,L-2-mercaptomethyl-3-guanidinoethyl-thipropanoic acid, a carboxypeptidase inhibitor
potato carboxypeptidase inhibitor
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fibrinolytic vulnerability and the contribution of thrombin activatable fibrinolysis inhibitor to fibrinolytic defenses in normal subjects are analysed: Plasma from 30 normal subjects is exposed to tissue factor/kaolin and tissue-type plasminogen activator. Prior to activation of coagulation, samples are either not exposed or exposed to potato carboxypeptidase inhibitor (25 microg/ml, a thrombin activatable fibrinolysis inhibitor). Thrombin activatable fibrinolysis inhibitor's inhibition decreases the time to onset of maximum fibrinolysis by 45%, increases the rate of maximum lysis by 50%, and decreases clot lysis time by 45%
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tick carboxypeptidase inhibitor
proteinaceous inhibitor TCI which is found in in the hematophagous ixodid tick Rhipicephalus bursa consists of tandem structurally similar small modules, an N-terminal and a C-terminal domain. TCI inhibits TFAIa mainly through its C-terminal domain. The C-terminal residue His75 is cleaved and the new C-terminus Leu74 approaches and contacts the TAFIa catalytic zinc ion through its carboxylate atoms. In addition to this contact, the C-terminal domain of TCI itneracts with TFAIa through 15 hydrogen bonds and 5 hydrophobic contacts
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UK-396082
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i.e. (S)-5-amino-2-((1-propyl-1H-imidazol-4-yl)methyl)pentanoic acid
additional information
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the enzyme is spontaneously inactivated by conformational changes
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additional information
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argatroban enhances fibrinolysis via a differential inhibition of thrombin-mediated activation of TAFI and factor XIII: Plasma is exposed to argatroban or heparin, with coagulation initiated with kaolin/tissue factor and fibrinolysis initiated with tissue plasminogen activator. Argatroban significantly decreases clot lysis time and increases the maximum rate of lysis compared with unexposed plasma, whereas heparin exposure only diminishs clot lysis time. Experiments with TAFI-deficient and factor XIII-deficient plasma demonstrate a sparing of thrombin-mediated factor XIII activation with concurrent inhibition of TAFI activation
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additional information
inhibition of the carboxypeptidase U system because of hemolysis results in an increase of lysis in functional fibrinolysis assays
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additional information
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the enzyme is spontaneously inactivated by conformational changes
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