Cloned (Comment) | Organism |
---|---|
gene ALDH1A1, recombinant expression of His-tagged enzyme in Escherichia coli strain BL21(DE3)pLys | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | [(5E)-2,4-dioxo-5-([4-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)methoxy]phenyl]methylidene)-1,3-thiazolidin-3-yl]acetic acid, a 2,4-thiazolidinedione-3-acetic acid derivative, is inactive as inhibitor; no inhibition of ALDH1A1 by [3-benzyl-5-(4-chlorophenyl)-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid | Homo sapiens | |
N,N'-(octane-1,8-diyl)bis(2,2-dichloroacetamide) | WIN 18,446; WIN 18,446, strong irreversible inhibition; WIN 18,446, weak inhibition | Homo sapiens | |
N,N-diethylaminobenzaldehyde | DEAB; DEAB; DEAB | Homo sapiens | |
[(5E)-2,4-dioxo-5-([4-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)methoxy]phenyl]methylidene)-1,3-thiazolidin-3-yl]acetic acid | a 2,4-thiazolidinedione-3-acetic acid derivative | Homo sapiens | |
[3-benzyl-5-(4-chlorophenyl)-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid | a 1-oxopyrimido[4,5-c]quinoline-2-acetic acid derivative; a 1-oxopyrimido[4,5-c]quinoline-2-acetic acid derivative and a non-competitive inhibitor of ALDH1A3 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
0.008 | - |
hexanal | pH 8.0, 25°C, recombinant enzyme | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytosol | - |
Homo sapiens | 5829 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
all-trans-retinal + H2O + NAD+ | Homo sapiens | - |
all-trans-retinoate + NADH + 2 H+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O94788 | - |
- |
Homo sapiens | P00352 | - |
- |
Homo sapiens | P47895 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3)pLys by nickel affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
A-549 cell | - |
Homo sapiens | - |
additional information | no activity in HL-60 cells | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
all-trans-retinal + H2O + NAD+ | - |
Homo sapiens | all-trans-retinoate + NADH + 2 H+ | - |
? | |
hexanal + H2O + NAD+ | - |
Homo sapiens | hexanoate + NADH + 2 H+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ALDH1A1 | - |
Homo sapiens |
Aldh1a2 | - |
Homo sapiens |
Aldh1a3 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NAD+ | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00007 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | N,N'-(octane-1,8-diyl)bis(2,2-dichloroacetamide) | |
0.00018 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | N,N-diethylaminobenzaldehyde | |
0.0012 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | [3-benzyl-5-(4-chlorophenyl)-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid | |
0.0035 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | [3-benzyl-5-(4-chlorophenyl)-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid | |
0.0054 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | [(5E)-2,4-dioxo-5-([4-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)methoxy]phenyl]methylidene)-1,3-thiazolidin-3-yl]acetic acid | |
0.0095 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | N,N-diethylaminobenzaldehyde | |
0.023 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | [(5E)-2,4-dioxo-5-([4-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)methoxy]phenyl]methylidene)-1,3-thiazolidin-3-yl]acetic acid | |
0.031 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | N,N'-(octane-1,8-diyl)bis(2,2-dichloroacetamide) | |
0.047 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | N,N-diethylaminobenzaldehyde | |
0.056 | - |
pH 8.0, 25°C, recombinant enzyme | Homo sapiens | N,N'-(octane-1,8-diyl)bis(2,2-dichloroacetamide) |
General Information | Comment | Organism |
---|---|---|
physiological function | the cytosolic isozymes ALDH1A1, ALDH1A2, and ALDH1A3 play important roles in cell signaling via oxidation of retinaldehyde to retinoic acid. In the cell, retinoic acid produced in the cytoplasm binds to cellular retinoic acid binding protein type II, and is transferred to the nucleus where it binds to heterodimers of retinoic acid receptor (RAR) and retinoid X receptor (RXR). Once activated, these receptor complexes bind to retinoic acid response elements (RAREs), which are regulatory sequences that induce gene transcription and modulate a wide range of biological processes, including cell proliferation, differentiation, cell cycle arrest and apoptosis | Homo sapiens |