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Literature summary extracted from

  • Ariza, A.; Vickers, T.J.; Greig, N.; Armour, K.A.; Dixon, M.J.; Eggleston, I.M.; Fairlamb, A.H.; Bond, C.S.
    Specificity of the trypanothione-dependent Leishmania major glyoxalase I: structure and biochemical comparison with the human enzyme (2006), Mol. Microbiol., 59, 1239-1248.
    View publication on PubMed

Application

EC Number Application Comment Organism
4.4.1.5 drug development mutually exclusive substrate specificities and substantial differences between the active sites of the Leishmania major and human GLO1 enzymes indicate that selective inhibition of LmGLO1 may be possible Leishmania major

Cloned(Commentary)

EC Number Cloned (Comment) Organism
4.4.1.5
-
 Leishmania major
4.4.1.5
-
 Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
4.4.1.5 to 2.0 A resolution, three protein dimers per asymmetric unit in spacegroup P21212, structural differences from both Escherichia coli GLO1 and human GLO1, loop between strands beta6 and beta7 is shortened, 15-residue C-terminal helix is not present in Escherichia coli GLO1, although a helix is observed at the C-terminus of human GLO1, it is in a different orientation and 10 residues shorter Leishmania major

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.4.1.5 S-2,4-dinitrophenylglutathione
-
 Homo sapiens
4.4.1.5 S-2,4-dinitrophenylglutathione
-
 Leishmania major
4.4.1.5 S-2,4-dinitrophenylglutathionylspermidine
-
 Homo sapiens
4.4.1.5 S-2,4-dinitrophenylglutathionylspermidine
-
 Leishmania major
4.4.1.5 S-4-bromobenzylglutathione
-
 Homo sapiens
4.4.1.5 S-4-bromobenzylglutathione
-
 Leishmania major
4.4.1.5 S-4-bromobenzylglutathionylspermidine linear competitive inhibitor Homo sapiens
4.4.1.5 S-4-bromobenzylglutathionylspermidine linear competitive inhibitor Leishmania major

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
4.4.1.5 0.042
-
 glutathione ethyl ester
-
 Homo sapiens
4.4.1.5 0.049
-
 glutathione
-
 Homo sapiens
4.4.1.5 0.053
-
 glutathione isopropyl ester
-
 Homo sapiens
4.4.1.5 0.064
-
 N-[3-[(4-aminobutyl)amino]propyl]-L-gamma-glutamyl-L-cysteinylglycine
-
 Leishmania major
4.4.1.5 0.071
-
 trypanothione
-
 Leishmania major
4.4.1.5 0.13
-
 trypanothione
-
 Homo sapiens
4.4.1.5 0.148
-
 N-[3-[(4-aminobutyl)amino]propyl]-L-gamma-glutamyl-L-cysteinylglycine
-
 Homo sapiens
4.4.1.5 0.3
-
 glutathione isopropyl ester
-
 Leishmania major
4.4.1.5 0.7
-
 glutathione ethyl ester
-
 Leishmania major
4.4.1.5 1.9
-
 glutathione
-
 Leishmania major

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
4.4.1.5 Ni2+
-
 Leishmania major
4.4.1.5 Zn2+
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
4.4.1.5 Homo sapiens Q04760
-
-
4.4.1.5 Leishmania major Q68RJ8
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
4.4.1.5
-
 Leishmania major
4.4.1.5
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.4.1.5 glutathione + methylglyoxal
-
 Homo sapiens S-D-lactoylglutathione
-
 ?
4.4.1.5 glutathione + methylglyoxal very poor substrate, specificity constant 280fold lower than of the N1-glutathionylspermidine Leishmania major S-D-lactoylglutathione
-
 ?
4.4.1.5 glutathione ethyl ester + methylglyoxal
-
 Homo sapiens ?
-
 ?
4.4.1.5 glutathione ethyl ester + methylglyoxal
-
 Leishmania major S-lactoylglutathionyl ethyl ester
-
 ?
4.4.1.5 glutathione ethyl ester + methylglyoxal
-
 Homo sapiens S-lactoylglutathionyl ethyl ester
-
 ?
4.4.1.5 glutathione isopropyl ester + methylglyoxal
-
 Leishmania major S-lactoylglutathionyl isopropyl ester
-
 ?
4.4.1.5 glutathione isopropyl ester + methylglyoxal
-
 Homo sapiens S-lactoylglutathionyl isopropyl ester
-
 ?
4.4.1.5 N1-glutathionylspermidine + methylglyoxal
-
 Leishmania major ?
-
 ?
4.4.1.5 N1-glutathionylspermidine + methylglyoxal specificity constant of N1-glutathionylspermidine 50fold less than of glutathione Homo sapiens ?
-
 ?
4.4.1.5 trypanothione + methylglyoxal
-
 Leishmania major S,S'-bis((R)-lactoyl)trypanothione
-
 ?
4.4.1.5 trypanothione + methylglyoxal
-
 Homo sapiens S,S'-bis((R)-lactoyl)trypanothione
-
 ?

Synonyms

EC Number Synonyms Comment Organism
4.4.1.5 Glo1
-
 Leishmania major
4.4.1.5 Glo1
-
 Homo sapiens
4.4.1.5 glyoxalase I
-
 Leishmania major
4.4.1.5 glyoxalase I
-
 Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
4.4.1.5 83
-
 N-[3-[(4-aminobutyl)amino]propyl]-L-gamma-glutamyl-L-cysteinylglycine
-
 Homo sapiens
4.4.1.5 104
-
 trypanothione
-
 Homo sapiens
4.4.1.5 164
-
 glutathione ethyl ester
-
 Homo sapiens
4.4.1.5 222
-
 glutathione isopropyl ester
-
 Homo sapiens
4.4.1.5 1070
-
 trypanothione
-
 Leishmania major
4.4.1.5 1170
-
 glutathione isopropyl ester
-
 Leishmania major
4.4.1.5 1360
-
 glutathione
-
 Homo sapiens
4.4.1.5 1590
-
 N-[3-[(4-aminobutyl)amino]propyl]-L-gamma-glutamyl-L-cysteinylglycine
-
 Leishmania major

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
4.4.1.5 0.000128
-
 S-4-bromobenzylglutathione
-
 Homo sapiens
4.4.1.5 0.000536
-
 S-4-bromobenzylglutathionylspermidine
-
 Leishmania major
4.4.1.5 0.0126
-
 S-4-bromobenzylglutathionylspermidine
-
 Homo sapiens
4.4.1.5 0.5
-
 S-2,4-dinitrophenylglutathione
-
 Leishmania major
4.4.1.5 0.5
-
 S-4-bromobenzylglutathione
-
 Leishmania major
4.4.1.5 0.645
-
 S-2,4-dinitrophenylglutathione
-
 Homo sapiens
4.4.1.5 0.669
-
 S-2,4-dinitrophenylglutathionylspermidine
-
 Leishmania major
4.4.1.5 0.915
-
 S-2,4-dinitrophenylglutathionylspermidine
-
 Homo sapiens