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Literature summary for 2.5.1.18 extracted from

  • Zompra, A.; Georgakis, N.; Pappa, E.; Thireou, T.; Eliopoulos, E.; Labrou, N.; Cordopatis, P.; Clonis, Y.
    Glutathione analogues as substrates or inhibitors that discriminate between allozymes of the MDR-involved human glutathione transferase P1-1 (2016), Biopolymers, 106, 330-344 .
    View publication on PubMed
Search for more literature for 2.5.1.18

Protein Variants

Protein Variants Comment Organism
I104V the mutant shows about 6fold increased activity compared to the wild type enzyme Homo sapiens
I104V/A113V the mutant shows about 3fold increased activity compared to the wild type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
gamma-Glu-Cys(Acm)-Gly 85.2% remaining activity at 0.0003 mM Homo sapiens
gamma-Glu-Cys(t-buthio)-Gly 85.6% remaining activity at 0.0003 mM Homo sapiens
gamma-Glu-Met-Gly 79.4% remaining activity at 0.0003 mM Homo sapiens
gamma-Glu-Thi-Gly 67.4% remaining activity at 0.0003 mM Homo sapiens
Gly-Cys-Hyp 87.4% remaining activity at 0.0003 mM Homo sapiens
Hyp-Cys-Ala 98.7% remaining activity at 0.0003 mM Homo sapiens
additional information not inhibited by acetyl-gamma-Glu-Cys-Gly, gamma-Glu-Cys-Aib, gamma-Glu-Cys-a-t-butyl-Gly, Sar-Cys(Trt)-Gly, Tic-Cys-Ala, and gamma-Glu-NMeCys-Gly Homo sapiens
pGlu-Cys(Trt)-Gly 82.3% remaining activity at 0.0003 mM Homo sapiens
Tic-Cys(Acm)-Gly 68.5% remaining activity at 0.0003 mM Homo sapiens
Tic-Cys-Aib 80.1% remaining activity at 0.0003 mM Homo sapiens
Tic-Cys-Sar 53% remaining activity at 0.0003 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.014
-
 gamma-Glu-Cys-Sar mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
0.033
-
 gamma-Glu-Cys-Sar mutant enzyme I104V, at pH 7.4 and 25°C Homo sapiens
0.074
-
 glutathione mutant enzyme I104V, at pH 7.4 and 25°C Homo sapiens
0.15
-
 glutathione mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
0.3
-
 glutathione wild type enzyme, at pH 7.4 and 25°C Homo sapiens
1.25
-
 Tic-Cys-Gly wild type enzyme, at pH 7.4 and 25°C Homo sapiens
1.48
-
 gamma-Glu-Cys-Aib mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
2.24
-
 acetyl-gamma-Glu-Cys-Gly mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
3.18
-
 gamma-Glu-Cys-Sar wild type enzyme, at pH 7.4 and 25°C Homo sapiens
3.22
-
 Hyp-Cys-Gly wild type enzyme, at pH 7.4 and 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09211
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-gamma-Glu-Cys-Gly + 1-chloro-2,4-dinitrobenzene substrate for mutant enzyme I104V/A113V Homo sapiens ?
-
 ?
gamma-Glu-Cys-Aib + 1-chloro-2,4-dinitrobenzene substrate for mutant enzyme I104V/A113V Homo sapiens ?
-
 ?
gamma-Glu-Cys-Nle + 1-chloro-2,4-dinitrobenzene 26.4% activity compared to glutathione Homo sapiens ?
-
 ?
gamma-Glu-Cys-Nva + 1-chloro-2,4-dinitrobenzene 16% activity compared to glutathione Homo sapiens ?
-
 ?
gamma-Glu-Cys-Sar + 1-chloro-2,4-dinitrobenzene 17% activity compared to glutathione Homo sapiens ?
-
 ?
glutathione + 1-chloro-2,4-dinitrobenzene 100% activity Homo sapiens chloride + 2,4-dinitrophenyl-glutathione
-
 ?
Hyp-Cys-Gly + 1-chloro-2,4-dinitrobenzene 39.5% activity compared to glutathione Homo sapiens ?
-
 ?
additional information the wild type enzyme shows no activity with acetyl-gamma-Glu-Cys-Gly, gamma-Glu-NMeCys-Gly, gamma-Glu-Cys-Aib, gamma-Glu-Cys-a-t-butyl-Gly, Tic-Cys-Ala, Hyp-Cys-Ala, Gly-Cys-Hyp, Tic-Cys-Aib, Tic-Cys(Acm)-Gly, and Tic-Cys-Sar Homo sapiens ?
-
-
NMe-Glu-Cys-Gly + 1-chloro-2,4-dinitrobenzene 3.9% activity compared to glutathione Homo sapiens ?
-
 ?
pGlu-Cys-Gly + 1-chloro-2,4-dinitrobenzene 11.5% activity compared to glutathione Homo sapiens ?
-
 ?
Pro-Cys-Gly + 1-chloro-2,4-dinitrobenzene 21.6% activity compared to glutathione Homo sapiens ?
-
 ?
Sar-Cys-Gly + 1-chloro-2,4-dinitrobenzene 15.8% activity compared to glutathione Homo sapiens ?
-
 ?
Tic-Cys-Gly + 1-chloro-2,4-dinitrobenzene 41.3% activity compared to glutathione Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
glutathione transferase P1-1
-
 Homo sapiens
GSTP1-1 isoform Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.31
-
 Tic-Cys-Gly wild type enzyme, at pH 7.4 and 25°C Homo sapiens
0.39
-
 gamma-Glu-Cys-Sar wild type enzyme, at pH 7.4 and 25°C Homo sapiens
0.53
-
 gamma-Glu-Cys-Sar mutant enzyme I104V, at pH 7.4 and 25°C Homo sapiens
0.56
-
 gamma-Glu-Cys-Sar mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
1.03
-
 acetyl-gamma-Glu-Cys-Gly mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
1.04
-
 Hyp-Cys-Gly wild type enzyme, at pH 7.4 and 25°C Homo sapiens
1.7
-
 glutathione wild type enzyme, at pH 7.4 and 25°C Homo sapiens
1.91
-
 gamma-Glu-Cys-Aib wild type enzyme, at pH 7.4 and 25°C Homo sapiens
2.29
-
 glutathione mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
2.52
-
 glutathione mutant enzyme I104V, at pH 7.4 and 25°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.12
-
 gamma-Glu-Cys-Sar wild type enzyme, at pH 7.4 and 25°C Homo sapiens
0.25
-
 Tic-Cys-Gly wild type enzyme, at pH 7.4 and 25°C Homo sapiens
0.32
-
 Hyp-Cys-Gly wild type enzyme, at pH 7.4 and 25°C Homo sapiens
0.46
-
 acetyl-gamma-Glu-Cys-Gly mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
1.29
-
 gamma-Glu-Cys-Aib wild type enzyme, at pH 7.4 and 25°C Homo sapiens
5.67
-
 glutathione wild type enzyme, at pH 7.4 and 25°C Homo sapiens
15.27
-
 glutathione mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens
16.07
-
 gamma-Glu-Cys-Sar mutant enzyme I104V, at pH 7.4 and 25°C Homo sapiens
34
-
 glutathione mutant enzyme I104V, at pH 7.4 and 25°C Homo sapiens
39.68
-
 gamma-Glu-Cys-Sar mutant enzyme I104V/A113V, at pH 7.4 and 25°C Homo sapiens