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Literature summary for 4.4.1.5 extracted from

  • Holewinski, R.J.; Creighton, D.J.
    Inhibition by active site directed covalent modification of human glyoxalase I (2014), Bioorg. Med. Chem., 22, 3301-3308.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression in Escherichia coli strain JM103 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-bromoacetoxy-1-(S-glutathionyl)-acetoxy butane competitive inhibition of GLO1, the inhibitor is able to covalently bind to the free sulfhydryl group of Cys60 in the hydrophobic binding pocket adjacent to the enzyme active site and partially inactivate the enzyme, no complete inhibition, binding structure analysis, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.182
-
methylglyoxal recombinant enzyme, pH 7.3, 25°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
20647
-
2 * 20647, sequence calculation, 2 * 21000, recombinant enzyme, SDS-PAGE Homo sapiens
21000
-
2 * 20647, sequence calculation, 2 * 21000, recombinant enzyme, SDS-PAGE Homo sapiens
42000
-
reombinant enzyme, native PAGE Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glutathione + methylglyoxal Homo sapiens
-
(R)-S-lactoylglutathione
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme from Escherichia coli strain JM103 by S-hexylglutathione affinity chromatography and gel filtration Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1580
-
purified recombinant enzyme, pH 7.3, 25°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione + methylglyoxal
-
Homo sapiens (R)-S-lactoylglutathione
-
?

Subunits

Subunits Comment Organism
homodimer 2 * 20647, sequence calculation, 2 * 21000, recombinant enzyme, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
Glo1
-
Homo sapiens
glyoxalase I
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1088
-
methylglyoxal recombinant enzyme, pH 7.3, 25°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.3 7.4 assay at Homo sapiens

General Information

General Information Comment Organism
metabolism glyoxalase I is the first enzyme of the methylglyoxal detoxification pathway Homo sapiens
physiological function the glyoxalase pathway is responsible for conversion of cytotoxic methylglyoxal to D-lactate. Methylglyoxal toxicity arises from its ability to form advanced glycation end products on proteins, lipids and DNA Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.006
-
methylglyoxal recombinant enzyme, pH 7.3, 25°C Homo sapiens