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Literature summary for 2.5.1.18 extracted from

  • Parker, L.J.; Ciccone, S.; Italiano, L.C.; Primavera, A.; Oakley, A.J.; Morton, C.J.; Hancock, N.C.; Bello, M.L.; Parker, M.W.
    The anti-cancer drug chlorambucil as a substrate for the human polymorphic enzyme glutathione transferase P1-1: kinetic properties and crystallographic characterisation of allelic variants (2008), J. Mol. Biol., 380, 131-144.
    View publication on PubMed
Search for more literature for 2.5.1.18

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with chlorambucil, hanging drop vapour diffusion method Homo sapiens

Protein Variants

Protein Variants Comment Organism
A113V wild type specific activity with 1-chloro-2,4-dinitrobenzene Homo sapiens
I104V decreased specific activity with 1-chloro-2,4-dinitrobenzene Homo sapiens
I104V/A113V decreased spcific activity with 1-chloro-2,4-dinitrobenzene Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
chlorambucil very poor inhibitor of the enzyme in contrast to ethacrynic acid Homo sapiens
Ethacrynic acid
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.002
-
 7-chloro-4-nitrobenz-2-oxa-1,3-diazole mutant enzyme I104V/A113V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.003
-
 glutathione mutant enzyme I104V/A113V, in the presence of cosubstrate 7-chloro-4-nitrobenz-2-oxa-1,3-diazole, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.004
-
 7-chloro-4-nitrobenz-2-oxa-1,3-diazole wild type enzyme, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.007
-
 7-chloro-4-nitrobenz-2-oxa-1,3-diazole mutant enzyme I104V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.007
-
 glutathione mutant enzyme I104V, in the presence of cosubstrate 7-chloro-4-nitrobenz-2-oxa-1,3-diazole, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.008
-
 glutathione wild type enzyme, in the presence of cosubstrate 7-chloro-4-nitrobenz-2-oxa-1,3-diazole, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.011
-
 7-chloro-4-nitrobenz-2-oxa-1,3-diazole mutant enzyme A113V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.014
-
 glutathione mutant enzyme A113V, in the presence of cosubstrate 7-chloro-4-nitrobenz-2-oxa-1,3-diazole, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.06
-
 Ethacrynic acid mutant enzyme104V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.08
-
 glutathione mutant enzyme I104V/A113V, in the presence of cosubstrate 1-chloro-2,4-dinitrobenzene, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.08
-
 Ethacrynic acid mutant enzyme104V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.09
-
 Ethacrynic acid mutant enzyme104V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.11
-
 glutathione mutant enzyme I104V, in the presence of cosubstrate 1-chloro-2,4-dinitrobenzene, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.13
-
 glutathione mutant enzyme A113V, in the presence of cosubstrate 1-chloro-2,4-dinitrobenzene, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.15
-
 glutathione wild type enzyme, in the presence of cosubstrate 1-chloro-2,4-dinitrobenzene, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.17
-
 glutathione mutant enzyme I104V, in the presence of cosubstrate ethacrynic acid, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.17
-
 glutathione wild type enzyme, in the presence of cosubstrate ethacrynic acid, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.2
-
 glutathione mutant enzyme I104V/A113V, in the presence of cosubstrate ethacrynic acid, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.21
-
 glutathione mutant enzyme A113V, in the presence of cosubstrate ethacrynic acid, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
0.21
-
 Ethacrynic acid wild type enzyme, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
1.2
-
 1-chloro-2,4-dinitrobenzene wild type enzyme, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
1.4
-
 1-chloro-2,4-dinitrobenzene mutant enzyme A113V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
2.3
-
 1-chloro-2,4-dinitrobenzene mutant enzyme I104V/A113V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens
2.9
-
 1-chloro-2,4-dinitrobenzene mutant enzyme I104V, in 0.1 M phosphate buffer at pH 6.5 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09211
-
-

Purification (Commentary)

Purification (Comment) Organism
GSTrap-Hp column chromatography Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.4
-
 mutant enzyme A113V, with ethacrynic acid Homo sapiens
1.7
-
 wild type enzyme, with ethacrynic acid Homo sapiens
1.8
-
 mutant enzyme I104V, with ethacrynic acid Homo sapiens
2.5
-
 mutant enzyme I104V, with 7-chloro-4-nitrobenz-2-oxa-1,3-diazole Homo sapiens
2.5
-
 mutant enzyme I104V/A113V, with ethacrynic acid Homo sapiens
3
-
 mutant enzyme I104V/A113V, with 7-chloro-4-nitrobenz-2-oxa-1,3-diazole Homo sapiens
3.7
-
 wild type enzyme, with 7-chloro-4-nitrobenz-2-oxa-1,3-diazole Homo sapiens
4
-
 mutant enzyme A113V, with 7-chloro-4-nitrobenz-2-oxa-1,3-diazole Homo sapiens
60
-
 mutant enzyme I104V, with 1-chloro-2,4-dinitrobenzene Homo sapiens
70
-
 mutant enzyme I104V/A113V, with 1-chloro-2,4-dinitrobenzene Homo sapiens
110
-
 mutant enzyme A113V, with 1-chloro-2,4-dinitrobenzene Homo sapiens
110
-
 wild type enzyme, with 1-chloro-2,4-dinitrobenzene Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione + 1-chloro-2,4-dinitrobenzene
-
 Homo sapiens S-(2,4-dinitrophenyl)glutathione + HCl
-
 ?
glutathione + 7-chloro-4-nitrobenz-2-oxa-1,3-diazole
-
 Homo sapiens ?
-
 ?
glutathione + chlorambucil
-
 Homo sapiens ?
-
 ?
glutathione + ethacrynic acid
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
glutathione transferase P1-1
-
 Homo sapiens
glutathione transferase Pi
-
 Homo sapiens
GST P1-1
-
 Homo sapiens

Temperature Range [°C]

Temperature Minimum [°C] Temperature Maximum [°C] Comment Organism
10 45
-
 Homo sapiens

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
50
-
 65.3% residual activity after 15 min at 50°C Homo sapiens