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Literature summary for 3.4.17.20 extracted from

  • Leurs, J.; Hendriks, D.
    Carboxypeptidase U (TAFIa): a metallocarboxypeptidase with a distinct role in haemostasis and a possible risk factor for thrombotic disease (2005), Thromb. Haemost., 94, 471-487.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene CPB2, gene mapping, genetic organization, DNA and amino acid sequence determination and analysis, regulation of enzyme expression involves the glucocorticoid receptor and the CCAAT/enhancer binding protein sites, polymorphisms at positions 325, 147, and 505 Homo sapiens

Protein Variants

Protein Variants Comment Organism
A505G naturally occurring polymorphism Homo sapiens
T147A naturally occurring polymorphism Homo sapiens
T325I naturally occurring polymorphism Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(6-aminopyridin-3-yl)-2-(1H-imidazol-4-yl)propanoic acid IC50: 0.000001 mM Homo sapiens
3-(6-aminopyridin-3-yl)-2-(sulfanylmethyl)propanoic acid
-
Homo sapiens
5-amino-2-[(1-propyl-1H-imidazol-4-yl)methyl]pentanoic acid
-
Homo sapiens
EF6265 i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.000001 mM Homo sapiens
epsilon-aminocaproic acid
-
Homo sapiens
GEMSA i.e. guanidinoethyl-thiopropanoic acid Homo sapiens
LCI leech carboxypeptidase inhibitor Homo sapiens
MERGETPA D,L-2-mercaptomethyl-3-guanidinoethyl-thipropanoic acid Homo sapiens
PCI-2KR i.e. peptide CKPAKNRC Homo sapiens
PTCI potato carboxypeptidase inhibitor Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ a metallocarboxypeptidase with a penta-coordinated zinc ion Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
anaphylatoxin C3a + H2O Homo sapiens inactivation of the inflammatory mediator ?
-
?
anaphylatoxin C5a + H2O Homo sapiens inactivation of the inflammatory mediator ?
-
?
additional information Homo sapiens the enzyme inhibits fibrinolysis and has a distinct role in haemostasis and a possible risk factor for thrombotic disease involving the polymorphism at position 325, overview, the plasminogen activation system plays a role in enzyme regulation ?
-
?
osteopontin + H2O Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein different glycosylation patterns dependent on the enzyme source Homo sapiens
proteolytic modification activation pathways overview, cleavage of the activation peptide from proCPU, in vitro catalyzed through thrombin, meizothrombin, plasmin, trypsin, or neutrophil elastase, only the thrombin cleaved enzyme is active, in vivo by the thrombin/thrombomodulin complex in a Ca2+-dependent manner, kinetics, overview, the plasminogen activation system, overview Homo sapiens

Purification (Commentary)

Purification (Comment) Organism
from plasma by a plasminogen affinity based method Homo sapiens

Reaction

Reaction Comment Organism Reaction ID
release of C-terminal Arg and Lys from a polypeptide catalytic mechanism and substrate specificity Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-
blood platelet
-
Homo sapiens
-
epithelium
-
Homo sapiens
-
liver
-
Homo sapiens
-
lung alveolar epithelium and macrophages, broncheal epithelium Homo sapiens
-
macrophage
-
Homo sapiens
-
additional information analysis of expression and distribution, overview, no expression in brain, kidney, placenta, and skeletal muscle Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
enzyme plasma concentration of healthy male persons, correlation of enzyme plasma concentration to cardiovascular diseases, overview Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
anaphylatoxin C3a + H2O
-
Homo sapiens ?
-
?
anaphylatoxin C3a + H2O inactivation of the inflammatory mediator Homo sapiens ?
-
?
anaphylatoxin C5a + H2O
-
Homo sapiens ?
-
?
anaphylatoxin C5a + H2O inactivation of the inflammatory mediator Homo sapiens ?
-
?
additional information the enzyme inhibits fibrinolysis and has a distinct role in haemostasis and a possible risk factor for thrombotic disease involving the polymorphism at position 325, overview, the plasminogen activation system plays a role in enzyme regulation Homo sapiens ?
-
?
osteopontin + H2O
-
Homo sapiens ?
-
?
osteopontin + H2O thrombin-cleaved substrate Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
carboxypeptidase U
-
Homo sapiens
CPU
-
Homo sapiens
proCPU
-
Homo sapiens
TAFIa
-
Homo sapiens

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
-
-
stable for several days Homo sapiens
37
-
body temperature, spontaneous decay, half-life 10 min Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
3-(6-aminopyridin-3-yl)-2-(sulfanylmethyl)propanoic acid
-
Homo sapiens
0.000001
-
LCI
-
Homo sapiens
0.00001
-
PCI-2KR
-
Homo sapiens
0.0001
-
5-amino-2-[(1-propyl-1H-imidazol-4-yl)methyl]pentanoic acid
-
Homo sapiens
0.0001 0.001 MERGETPA
-
Homo sapiens
0.001 0.1 GEMSA
-
Homo sapiens
110
-
epsilon-aminocaproic acid
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.000001 mM Homo sapiens EF6265
0.000001
-
IC50: 0.000001 mM Homo sapiens 3-(6-aminopyridin-3-yl)-2-(1H-imidazol-4-yl)propanoic acid