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Literature summary for 4.4.1.5 extracted from

  • More, S.S.; Vince, R.
    A metabolically stable tight-binding transition-state inhibitor of glyoxalase-I (2006), Bioorg. Med. Chem. Lett., 16, 6039-6042.
    View publication on PubMed

Application

Application Comment Organism
drug development design of a metabolically stable glyoxalase-I inhibitor, which may be useful in potentiating the antitumor activity of alpha-ketoaldehydes Saccharomyces cerevisiae

Inhibitors

Inhibitors Comment Organism Structure
L-gamma-glutamyl-S-[(4-bromophenyl)(hydroxy)carbamoyl]-L-cysteinylglycine hydroxamic acid-based transition state inhibitor, unstable toward gamma-glutamyltranspeptidase Saccharomyces cerevisiae
N-[[(2S)-2-amino-2-carboxyethyl]carbamoyl]-S-[(4-bromophenyl)(hydroxy)carbamoyl]-L-cysteinylglycine tight-binding competitive inhibitor, stable toward gamma-glutamyltranspeptidase Saccharomyces cerevisiae
S-p-bromobenzyl glutathione competitive inhibitor, unstable toward gamma-glutamyltranspeptidase Saccharomyces cerevisiae

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.35
-
glutathione
-
Saccharomyces cerevisiae
0.35
-
methylglyoxal
-
Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Saccharomyces cerevisiae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione + methylglyoxal
-
Saccharomyces cerevisiae S-D-lactoylglutathione
-
?

Synonyms

Synonyms Comment Organism
Glx-I
-
Saccharomyces cerevisiae
glyoxalase-I
-
Saccharomyces cerevisiae

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.6
-
-
Saccharomyces cerevisiae

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00219
-
N-[[(2S)-2-amino-2-carboxyethyl]carbamoyl]-S-[(4-bromophenyl)(hydroxy)carbamoyl]-L-cysteinylglycine
-
Saccharomyces cerevisiae