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Literature summary for 4.4.1.5 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
Search for more literature for 4.4.1.5

Application

Application Comment Organism
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)

Cloned (Comment) Organism
-
 Leishmania major
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
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

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

KM Value [mM]

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

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04760
-
-
Leishmania major Q68RJ8
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Leishmania major
-
 Homo sapiens

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

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

Ki Value [mM]

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