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Literature summary extracted from

  • Tsirulnikov, K.; Abuladze, N.; Bragin, A.; Faull, K.; Cascio, D.; Damoiseaux, R.; Schibler, M.J.; Pushkin, A.
    Inhibition of aminoacylase 3 protects rat brain cortex neuronal cells from the toxicity of 4-hydroxy-2-nonenal mercapturate and 4-hydroxy-2-nonenal (2012), Toxicol. Appl. Pharmacol., 263, 303-314.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.5.1.114 recombinant expression of the enzyme in Escherichia coli Mus musculus
3.5.1.114 recombinant expression of the enzyme in Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.1.114 2-((E)-[(4H-1,2,4-triazol-4-yl)imino]methyl)-1-benzothiophene-3-ol
-
Rattus norvegicus
3.5.1.114 2-(4-ethoxyphenyl)-2-methylsuccinic acid
-
Homo sapiens
3.5.1.114 2-(4-ethoxyphenyl)-2-methylsuccinic acid
-
Mus musculus
3.5.1.114 2-(4-ethoxyphenyl)-2-methylsuccinic acid
-
Rattus norvegicus
3.5.1.114 2-([(3-fluoro-4-methoxyphenyl)methyl]sulfanyl)-1-methyl-1H-benzimidazole-5-sulfonamide
-
Rattus norvegicus
3.5.1.114 2-([2-chloro-4-(thiocyanato)phenyl]carbamoyl)benzoic acid
-
Rattus norvegicus
3.5.1.114 2-[(1,3-benzothiazol-2-yl)sulfanyl]ethan-1-amine
-
Rattus norvegicus
3.5.1.114 clioquinol
-
Rattus norvegicus
3.5.1.114 ebselen
-
Homo sapiens
3.5.1.114 ebselen
-
Mus musculus
3.5.1.114 ebselen
-
Rattus norvegicus
3.5.1.114 Ibuprofen
-
Mus musculus
3.5.1.114 additional information the enzyme is a metalloenzyme that is inactivated by metal chelating compounds. Molecular docking, overview Homo sapiens
3.5.1.114 additional information the enzyme is a metalloenzyme that is inactivated by metal chelating compounds. Molecular docking, overview Mus musculus
3.5.1.114 additional information the enzyme is a metalloenzyme that is inactivated by metal chelating compounds. Molecular docking, overview Rattus norvegicus
3.5.1.114 N-(2,3,5-trichloro-4-oxocyclohexa-2,5-dien-1-ylidene)benzenesulfonamide
-
Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.5.1.114 additional information
-
additional information Michaelis-Menten kinetics Mus musculus
3.5.1.114 0.2
-
4-hydroxy-2-nonenal mercapturate pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.3
-
N-acetyl-L-tyrosine pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 0.45
-
N-acetyl-L-tyrosine pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.53
-
4-hydroxy-2-nonenal mercapturate pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 0.56
-
N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 0.71
-
acrolein mercapturate pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 0.82
-
acrolein mercapturate pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 1.3
-
N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine pH and temperature not specified in the publication, absence of Co2+ Mus musculus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.5.1.114 Co2+ metalloenzyme, highly activating Mus musculus
3.5.1.114 Co2+ metalloenzyme, highly activating Rattus norvegicus
3.5.1.114 Co2+ metalloenzyme, highly activating Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.11.2 Mus musculus
-
-
-
3.4.19.9 Mus musculus
-
-
-
3.5.1.114 Homo sapiens Q96HD9
-
-
3.5.1.114 Mus musculus Q91XE4
-
-
3.5.1.114 Rattus norvegicus Q5M876
-
-
3.5.1.114 Rattus norvegicus Wistar Q5M876
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.5.1.114 recombinant enzyme from Escherichia coli to homogeneity Mus musculus
3.5.1.114 recombinant enzyme from Escherichia coli to homogeneity Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.11.2 brain
-
Mus musculus
-
3.4.19.9 brain
-
Mus musculus
-
3.5.1.114 blood vessel
-
Mus musculus
-
3.5.1.114 blood vessel
-
Rattus norvegicus
-
3.5.1.114 blood vessel
-
Homo sapiens
-
3.5.1.114 brain cortex
-
Mus musculus
-
3.5.1.114 brain cortex
-
Rattus norvegicus
-
3.5.1.114 brain cortex
-
Homo sapiens
-
3.5.1.114 hippocampus
-
Rattus norvegicus
-
3.5.1.114 neuron
-
Rattus norvegicus
-
3.5.1.114 neuron
-
Homo sapiens
-
3.5.1.114 neuron mainly Mus musculus
-
3.5.1.114 neuronal cell
-
Mus musculus
-
3.5.1.114 neuronal cell
-
Homo sapiens
-
3.5.1.114 neuronal cell hippocampal Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.11.2 4-hydroxy-2-nonenal-[Cys-Gly] conjugate + H2O
-
Mus musculus 4-hydroxy-2-nonenal-[L-Cys] conjugate + glycine
-
?
3.4.19.9 4-hydroxy-2-nonenal-glutathione conjugate + H2O
-
Mus musculus 4-hydroxy-2-nonenal-[Cys-Gly] conjugate + L-glutamate
-
?
3.5.1.114 4-hydroxy-2-nonenal mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Mus musculus ?
-
?
3.5.1.114 4-hydroxy-2-nonenal mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Rattus norvegicus ?
-
?
3.5.1.114 4-hydroxy-2-nonenal mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Homo sapiens ?
-
?
3.5.1.114 4-hydroxy-2-nonenal mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Rattus norvegicus Wistar ?
-
?
3.5.1.114 acrolein mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Mus musculus ?
-
?
3.5.1.114 acrolein mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Rattus norvegicus ?
-
?
3.5.1.114 acrolein mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Homo sapiens ?
-
?
3.5.1.114 acrolein mercapturate + H2O substrate of aminoacylase 3, not aminoacylase 1, deacetylation Rattus norvegicus Wistar ?
-
?
3.5.1.114 N-acetyl-L-tyrosine + H2O
-
Mus musculus acetate + L-tyrosine
-
?
3.5.1.114 N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine + H2O
-
Mus musculus acetate + S-(1,2-dichlorovinyl)-L-cysteine
-
?

Synonyms

EC Number Synonyms Comment Organism
3.4.11.2 dipeptidase
-
Mus musculus
3.4.11.2 DP
-
Mus musculus
3.5.1.114 AA3
-
Mus musculus
3.5.1.114 AA3
-
Rattus norvegicus
3.5.1.114 AA3
-
Homo sapiens
3.5.1.114 aminoacylase 3
-
Mus musculus
3.5.1.114 aminoacylase 3
-
Rattus norvegicus
3.5.1.114 aminoacylase 3
-
Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.5.1.114 0.13
-
N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.27
-
4-hydroxy-2-nonenal mercapturate pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.28
-
N-acetyl-L-tyrosine pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.4
-
acrolein mercapturate pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 1.09
-
N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 1.67
-
4-hydroxy-2-nonenal mercapturate pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 2.28
-
N-acetyl-L-tyrosine pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 3.03
-
acrolein mercapturate pH and temperature not specified in the publication, presence of Co2+ Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.1.114 0.00000063
-
pH and temperature not specified in the publication Rattus norvegicus 2-(4-ethoxyphenyl)-2-methylsuccinic acid
3.5.1.114 0.0000032
-
pH and temperature not specified in the publication Rattus norvegicus N-(2,3,5-trichloro-4-oxocyclohexa-2,5-dien-1-ylidene)benzenesulfonamide
3.5.1.114 0.00004
-
pH and temperature not specified in the publication Rattus norvegicus 2-([2-chloro-4-(thiocyanato)phenyl]carbamoyl)benzoic acid
3.5.1.114 0.000079
-
pH and temperature not specified in the publication Rattus norvegicus 2-([(3-fluoro-4-methoxyphenyl)methyl]sulfanyl)-1-methyl-1H-benzimidazole-5-sulfonamide
3.5.1.114 0.0016
-
pH and temperature not specified in the publication Rattus norvegicus 2-[(1,3-benzothiazol-2-yl)sulfanyl]ethan-1-amine
3.5.1.114 0.0101
-
pH and temperature not specified in the publication Rattus norvegicus clioquinol
3.5.1.114 0.063
-
pH and temperature not specified in the publication Rattus norvegicus 2-((E)-[(4H-1,2,4-triazol-4-yl)imino]methyl)-1-benzothiophene-3-ol
3.5.1.114 10
-
pH and temperature not specified in the publication Rattus norvegicus ebselen

General Information

EC Number General Information Comment Organism
3.5.1.114 malfunction aminoacylase 3 inhibition completely protects rat brain cortex neurons expressing the enzyme from the toxicity of 4-hydroxy-2-nonenal-mercapturate. 4-hydroxy-2-nonenal-cysteine is also neurotoxic and its toxicity is mostly prevented by a beta-lyase inhibitor, aminooxyacetate Mus musculus
3.5.1.114 malfunction aminoacylase 3 inhibition completely protects rat brain cortex neurons expressing the enzyme from the toxicity of 4-hydroxy-2-nonenal-mercapturate. 4-hydroxy-2-nonenal-cysteine is also neurotoxic and its toxicity is mostly prevented by a beta-lyase inhibitor, aminooxyacetate Rattus norvegicus
3.5.1.114 malfunction aminoacylase 3 inhibition completely protects rat brain cortex neurons expressing the enzyme from the toxicity of 4-hydroxy-2-nonenal-mercapturate. 4-hydroxy-2-nonenal-cysteine is also neurotoxic and its toxicity is mostly prevented by a beta-lyase inhibitor, aminooxyacetate Homo sapiens
3.5.1.114 physiological function the enzyme cleaves the conjugates 4-hydroxy-2-nonenal mercapturate and acrolein mercapturate formed by reaction with glutathione for detoxification in the GSH-conjugation pathway, overview. Aminoacylase 3 is involved in the neurotoxicity of the compounds 4-hydroxy-2-nonenal and acrolein Mus musculus
3.5.1.114 physiological function the enzyme cleaves the conjugates 4-hydroxy-2-nonenal mercapturate and acrolein mercapturate formed by reaction with glutathione for detoxification in the GSH-conjugation pathway, overview. Aminoacylase 3 is involved in the neurotoxicity of the compounds 4-hydroxy-2-nonenal and acrolein Rattus norvegicus
3.5.1.114 physiological function the enzyme cleaves the conjugates 4-hydroxy-2-nonenal mercapturate and acrolein mercapturate formed by reaction with glutathione for detoxification in the GSH-conjugation pathway, overview. Aminoacylase 3 is involved in the neurotoxicity of the compounds 4-hydroxy-2-nonenal and acrolein Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.5.1.114 0.1
-
N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.49
-
acrolein mercapturate pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 0.62
-
N-acetyl-L-tyrosine pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 1.35
-
4-hydroxy-2-nonenal mercapturate pH and temperature not specified in the publication, absence of Co2+ Mus musculus
3.5.1.114 1.93
-
N-acetyl-S-(1,2-dichlorovinyl)-L-cysteine pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 3.15
-
4-hydroxy-2-nonenal mercapturate pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 4.27
-
acrolein mercapturate pH and temperature not specified in the publication, presence of Co2+ Mus musculus
3.5.1.114 7.6
-
N-acetyl-L-tyrosine pH and temperature not specified in the publication, presence of Co2+ Mus musculus