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Literature summary for 4.4.1.5 extracted from

  • Takasawa, R.; Takahashi, S.; Saeki, K.; Sunaga, S.; Yoshimori, A.; Tanuma, S.
    Structure-activity relationship of human GLO I inhibitory natural flavonoids and their growth inhibitory effects (2008), Bioorg. Med. Chem., 16, 3969-3975.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
baicalein 79% inhibition of rhGLO I at 0.1 mM Homo sapiens
Baicalin 30% inhibition of rhGLO I at 0.1 mM Homo sapiens
hyperin below 5% inhibition of rhGLO I at 0.1 mM Homo sapiens
kaempferol 60% inhibition of rhGLO I at 0.1 mM Homo sapiens
luteolin 90% inhibition of rhGLO I at 0.1 mM Homo sapiens
myricetin 75% inhibition of rhGLO I at 0.1 mM Homo sapiens
naringenin 50% inhibition of rhGLO I at 0.1 mM Homo sapiens
oroxylin A 140% inhibition of rhGLO I at 0.1 mM Homo sapiens
quercetin 78% inhibition of rhGLO I at 0.1 mM Homo sapiens
S-p-bromobenzylglutathione 55% inhibition of rhGLO I at 0.1 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04760
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HL-60 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
methylglyoxal + glutathione
-
Homo sapiens S-((R)-lactoyl)glutathione determined monitoring the increase in absorbance at 240 nm for 5 min at 25°C, pH 7.0 ?

Synonyms

Synonyms Comment Organism
GLO I
-
Homo sapiens
glyoxalase I
-
Homo sapiens
rhGLO I His-tagged GLO I protein Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00056
-
indicate that the hydroxy groups at the B ring of flavonoids contribute to the human GLO I inhibitory activity of the flavonoid compounds at 25°C, pH 7.0 Homo sapiens myricetin
0.0032
-
indicate that the hydroxy groups at the B ring of flavonoids contribute to the human GLO I inhibitory activity of the flavonoid compounds at 25°C, pH 7.0 Homo sapiens quercetin
0.007
-
indicate that the hydroxy groups at the B ring of flavonoids contribute to the human GLO I inhibitory activity of the flavonoid compounds at 25°C, pH 7.0 Homo sapiens luteolin
0.011
-
indicate that the hydroxy groups at the B ring of flavonoids contribute to the human GLO I inhibitory activity of the flavonoid compounds at 25°C, pH 7.0 Homo sapiens baicalein
0.0206
-
indicate that the hydroxy groups at the B ring of flavonoids contribute to the human GLO I inhibitory activity of the flavonoid compounds at 25°C, pH 7.0 Homo sapiens kaempferol
0.023
-
calculated, effectively inhibits rhGLO I at 25°C, pH 7.0 Homo sapiens S-p-bromobenzylglutathione