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Information on EC 3.4.17.20 - Carboxypeptidase U and Organism(s) Rattus norvegicus and UniProt Accession Q9EQV9
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3.4.17.20 Carboxypeptidase USpecify your search results
Word Map
- 3.4.17.20
- plasminogen
- coagulation
- clot
-
fibrinolytic
- thrombosis
- thrombomodulin
- plasmin
- fibrinogen
- pai-1
-
bleeding
- inhibitor-1
-
antifibrinolytic
-
hemostatic
- prothrombin
- zymogen
- venous
-
anticoagulant
- thromboembolism
-
tissue-type
-
d-dimers
-
hypofibrinolysis
-
profibrinolytic
-
thrombolytic
- thrombin-thrombomodulin
-
hypercoagulable
-
procoagulant
- c5a
- antithrombin
- thrombus
-
prothrombotic
-
thrombin-antithrombin
-
thrombin-mediated
- coagulopathy
-
plasmin-antiplasmin
-
haemostasis
- thromboplastin
- medicine
- antiplasmin
- alpha2-antiplasmin
-
fxiii
- metallocarboxypeptidase
- anaphylatoxins
- molecular biology
- pharmacology
-
plasmin-mediated
- thrombophilia
-
thrombelastography
-
activator-induced
-
thrombin-dependent
- rfviia
-
t-pa-induced
-
thrombin-cleaved
-
euglobulin
- diagnostics
The taxonomic range for the selected organisms is: Rattus norvegicus
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Synonyms
tafia, thrombin-activatable fibrinolysis inhibitor, thrombin activatable fibrinolysis inhibitor, procpu, procarboxypeptidase b, carboxypeptidase u, thrombin-activable fibrinolysis inhibitor, procarboxypeptidase u, carboxypeptidase b2, plasma carboxypeptidase b, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
Arginine carboxypeptidase
-
-
-
-
Carboxypeptidase B, pro-
-
-
-
-
Carboxypeptidase R
Carboxypeptidase-U
-
-
-
-
CPU
-
-
-
-
Plasma carboxypeptidase B
pro-pCPB
-
-
-
-
Procarboxypeptidase B
-
-
-
-
pTAFI
-
-
-
-
rTAFI
-
-
-
-
TAFI
TAFIa
Thrombin-activable fibrinolysis inhibitor
-
-
-
-
Carboxypeptidase R
-
-
-
-
Plasma carboxypeptidase B
-
-
-
-
TAFI
-
-
-
-
TAFIa
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
156621-18-0
-
37329-68-3
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
additional information
?
-
-
pro-carboxypeptidase R production is increased under inflammatory conditions
-
?
additional information
?
-
-
the enzyme down-regulates fibrinolysis by removing carboxy-terminal lysine residues, which are ligands for plasminogen and tissue-type plasminogen activator, from partially degraded fibrin, pharmacological profile and pathphysiological role of the enzyme in rat thrombolysis
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
additional information
?
-
-
pro-carboxypeptidase R production is increased under inflammatory conditions
-
?
additional information
?
-
-
the enzyme down-regulates fibrinolysis by removing carboxy-terminal lysine residues, which are ligands for plasminogen and tissue-type plasminogen activator, from partially degraded fibrin, pharmacological profile and pathphysiological role of the enzyme in rat thrombolysis
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
EF6265
-
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
-
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
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00000389
EF6265
Rattus norvegicus
-
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
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
electroluminescence assay. The high sensitivity of the assay allows the determination of the activatable levels of TAFI in human and other animal plasma in presence of epsilon-aminocaproic acid, an active-site inhibitor that stabilizes TAFIa
additional information
-
in vivo arteriovenous shunt thrombosis model, ex vivo clot lysis assay
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
hepatocytic expression, pro-carboxypeptidase R mRNA is detected only in liver
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). CBPB2_RAT
422
0
48827
Swiss-Prot
Secretory Pathway (Reliability: 3)
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
proteolytic modification
proteolytic modification
-
carboxypeptidase R is generated from pro-carboxypeptidase R by trypsin-like enzymes such as thrombin. Carboxypeptidase R regulates not only inflammatory peptides but also restricts fibrinolysis
proteolytic modification
-
procarboxypeptidase R is generated from pro-carboxypeptidase R, a plasma zymogen, by proteolytic enzymes such as thrombin, thrombin-thrombomodulin complex and plasmin
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
25
-
half-life of carboxypeptidase R: 36 min, half-life of thrombin/thrombomodulin complex activated carboxypeptidase R: 27 min
37
-
half-life of carboxypeptidase R: 16 min, half-life of thrombin/thrombomodulin complex activated carboxypeptidase R: 13 min
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
development of a method to isolate in situ activated TAFIa from serum in presence of epsilon-aminocaproic acid
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
results provide evidence for a role of TAFI in arterial thrombosis in rats and suggest that TAFI inhibition could be explored as an attractive target for the development of new antithrombotic drugs
medicine
-
TAFI plays an important role in the deterioration of organ dysfunction in sepsis and the inhibitor of TAFIa protects against sepsis-induced tissue damage through regulation of fibrinolysis and inflammation
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Mao, S.S.; Colussi, D.; Bailey, C.M.; Bosserman, M.; Burlein, C.; Gardell, S.J.; Carroll, S.S.
Electrochemiluminescence assay for basic carboxypeptidases: inhibition of basic carboxypeptidases and activation of thrombin-activatable fibrinolysis inhibitor
Anal. Biochem.
319
159-170
2003
Chlorocebus aethiops, Canis lupus familiaris, Homo sapiens, Macaca mulatta, Rattus norvegicus
Suzuki, K.; Muto, Y.; Fushihara, K.; Kanemoto, K.; Iida, H.; Sato, E.; Kikuchi, C.; Matsushima, T.; Kato, E.; Nomoto, M.; Yoshioka, S.; Ishii, H.
Enhancement of fibrinolysis by EF6265 [(S)-7-amino-2-[[[(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxypho sphinoyl] methyl]heptanoic acid], a specific inhibitor of plasma carboxypeptidase B
J. Pharmacol. Exp. Ther.
309
607-615
2004
Homo sapiens, Rattus norvegicus
Kato, T.; Akatsu, H.; Sato, T.; Matsuo, S.; Yamamoto, T.; Campbell, W.; Hotta, N.; Okada, N.; Okada, H.
Molecular cloning and partial characterization of rat procarboxypeptidase R and carboxypeptidase N
Microbiol. Immunol.
44
719-728
2000
Rattus norvegicus
Komura, H.; Shimomura, Y.; Yumoto, M.; Katsuya, H.; Okada, N.; Okada, H.
Heat stability of carboxypeptidase R of experimental animals
Microbiol. Immunol.
46
217-223
2002
Cavia porcellus, Homo sapiens, Oryctolagus cuniculus, Rattus norvegicus
Bouma, B.N.; Marx, P.F.; Mosnier, L.O.; Meijers, J.C.
Thrombin-activatable fibrinolysis inhibitor (TAFI, plasma procarboxypeptidase B, procarboxypeptidase R, procarboxypeptidase U)
Thromb. Res.
101
329-354
2001
Papio sp., Canis lupus familiaris, Cavia porcellus, Oryctolagus cuniculus, Homo sapiens, Mus musculus, Rattus norvegicus, Sus scrofa
Muto, Y.; Suzuki, K.; Iida, H.; Sakakibara, S.; Kato, E.; Itoh, F.; Kakui, N.; Ishii, H.
EF6265, a novel thrombin-activatable fibrinolysis inhibitor-a inhibitor, protects against sepsis-induced organ dysfunction in rats
Crit. Care Med.
37
1744-1749
2009
Rattus norvegicus
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