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Literature summary for 3.5.1.114 extracted from

  • Tsirulnikov, K.; Duarte, S.; Ray, A.; Datta, N.; Zarrinpar, A.; Hwang, L.; Faull, K.; Pushkin, A.; Kurtz, I.
    Aminoacylase 3 is a new potential marker and therapeutic target in hepatocellular carcinoma (2018), J. Cancer, 9, 1-12 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.114

Application

Application Comment Organism
medicine expression is significantly elevated in the livers of hepatocellular carcinoma patients and hepatocellular carcinoma cell lines. Treatment of HepG2 cells with AA3 inhibitors, and HepG2 and HuH7 with AA3 siRNA significantly decreases Ras membrane association and is toxic to these HCC cell lines. AA3 inhibition may be an effective approach in the therapy of hepatocellular carcinoma and elevated AA3 expression in hepatocellular carcinoma is potentially an important diagnostic marker Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
N-terminally 6His-tagged enzyme is expressed in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-phenyl-4H-1,3-benzothiazin-4-one
-
 Homo sapiens
2-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1-methyl-1Hbenzimidazole-5-sulfonamide
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.025
-
 N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine pH 7.5, 37°C Homo sapiens
0.14
-
 N-acetyl-S-geranylgeranyl-L-cysteine pH 7.5, 37°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
35000
-
 SDS-PAGE Homo sapiens
100000
-
 SDS-PAGE, the 90000-100000 Da band is detected in most hepatocellular carcinoma cell lines but not in normal hepatocytes Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
N-acetyl-S-geranylgeranyl-L-cysteine + H2O Homo sapiens the 90000-100000 Da AA3 form (that is detected in most hepatocellular carcinoma cell lines but not in normal hepatocytes) is functionally active and together with the normal 35000 Da AA3 form mediates the deacetylation of N-acetylfarnesylcysteine and N-acetylgeranylgeranylcysteine 3-geranylgeranyl-L-cysteine + acetate
-
 ?
N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine + H2O Homo sapiens the 90000-100000 Da AA3 form (that is detected in most hepatocellular carcinoma cell lines but not in normal hepatocytes) is functionally active and together with the normal 35000 Da AA3 form mediates the deacetylation of N-acetylfarnesylcysteine and N-acetylgeranylgeranylcysteine S-[(2E,6E)-farnesyl]-L-cysteine + acetate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q96HD9
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte AA3 expression in the hepatocellular carcinoma cell lines is 5 to 20 times greater than in normal primary hepatocytes Homo sapiens
-
hepatoma cell line AA3 expression in the hepatocellular carcinoma cell lines is 5 to 20 times greater than in normal primary hepatocytes Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-acetyl-S-geranylgeranyl-L-cysteine + H2O
-
 Homo sapiens 3-geranylgeranyl-L-cysteine + acetate
-
 ?
N-acetyl-S-geranylgeranyl-L-cysteine + H2O the 90000-100000 Da AA3 form (that is detected in most hepatocellular carcinoma cell lines but not in normal hepatocytes) is functionally active and together with the normal 35000 Da AA3 form mediates the deacetylation of N-acetylfarnesylcysteine and N-acetylgeranylgeranylcysteine Homo sapiens 3-geranylgeranyl-L-cysteine + acetate
-
 ?
N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine + H2O
-
 Homo sapiens S-[(2E,6E)-farnesyl]-L-cysteine + acetate
-
 ?
N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine + H2O the 90000-100000 Da AA3 form (that is detected in most hepatocellular carcinoma cell lines but not in normal hepatocytes) is functionally active and together with the normal 35000 Da AA3 form mediates the deacetylation of N-acetylfarnesylcysteine and N-acetylgeranylgeranylcysteine Homo sapiens S-[(2E,6E)-farnesyl]-L-cysteine + acetate
-
 ?

Subunits

Subunits Comment Organism
monomer 1 * 35000, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
AA3
-
 Homo sapiens
aminoacylase 3
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2
-
 N-acetyl-S-[(2E,6E)-farnesyl]-L-cysteine pH 7.5, 37°C Homo sapiens
7.2
-
 N-acetyl-S-geranylgeranyl-L-cysteine pH 7.5, 37°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

Expression

Organism Comment Expression
Homo sapiens expression is significantly elevated in the livers of hepatocellular carcinoma patients and hepatocellular carcinoma cell lines up