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Literature summary for 2.7.1.1 extracted from

  • Sanz-Rodriguez, C.E.; Concepcion, J.L.; Pekerar, S.; Oldfield, E.; Urbina, J.A.
    Bisphosphonates as inhibitors of Trypanosoma cruzi hexokinase: kinetic and metabolic studies (2007), J. Biol. Chem., 282, 12377-12387.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2-pyridin-4-ylethane-1,1-diyl)bis(phosphonic acid) mixed to non-competitive inhibitors against ATP, non-competitive against D-glucose Trypanosoma cruzi
(3-bromo-phenyl)-aminomethylene-1,1-bisphosphonate
-
Trypanosoma cruzi
(9-ethyl-9H-3-carbazolyl)-aminomethylene-1,1-bisphosphonate
-
Trypanosoma cruzi
2-(pyridin-4-yl)-1-hydroxyethane-1,1-bisphosphonate
-
Trypanosoma cruzi
diphosphate non-competitive inhibition towards ATP, mixed-type towards D-glucose; non-competitive inhibitor Trypanosoma cruzi
additional information enzyme is not affected by D-glucose 6-phosphate; TcHK is not affected by D-glucose 6-phosphate Trypanosoma cruzi
[[(3-bromophenyl)amino]methylene]bis(phosphonic acid) mixed to non-competitive inhibitors against ATP, competitive against D-glucose Trypanosoma cruzi
[[(9-ethyl-9H-carbazol-3-yl)amino]methylene]bis(phosphonic acid) mixed to non-competitive inhibitors against ATP, competitive against D-glucose Trypanosoma cruzi

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.03
-
ATP
-
Trypanosoma cruzi
0.463
-
D-glucose
-
Trypanosoma cruzi

Localization

Localization Comment Organism GeneOntology No. Textmining
glycosome
-
Trypanosoma cruzi 20015
-

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + D-glucose
-
Trypanosoma cruzi ADP + D-glucose 6-phosphate
-
?

Synonyms

Synonyms Comment Organism
ATP-dependent hexokinase
-
Trypanosoma cruzi
TcHK
-
Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0004
-
(3-bromo-phenyl)-aminomethylene-1,1-bisphosphonate varied substrate is D-glucose, in the presence of 1 mM ATP and 3 mM MgCl2, Kis Trypanosoma cruzi
0.0005
-
(9-ethyl-9H-3-carbazolyl)-aminomethylene-1,1-bisphosphonate varied substrate is D-glucose, in the presence of 1 mM ATP and 3 mM MgCl2, Kis Trypanosoma cruzi
0.0006
-
(3-bromo-phenyl)-aminomethylene-1,1-bisphosphonate varied substrate is ATP, in the presence of 2 mM D-glucose and 3 mM MgCl2, Kis Trypanosoma cruzi
0.0012
-
(3-bromo-phenyl)-aminomethylene-1,1-bisphosphonate varied substrate is ATP, in the presence of 2 mM D-glucose and 3 mM MgCl2, Kii Trypanosoma cruzi
0.0017
-
(9-ethyl-9H-3-carbazolyl)-aminomethylene-1,1-bisphosphonate varied substrate is ATP, in the presence of 2 mM D-glucose and 3 mM MgCl2, Kis Trypanosoma cruzi
0.0028
-
(9-ethyl-9H-3-carbazolyl)-aminomethylene-1,1-bisphosphonate varied substrate is ATP, in the presence of 2 mM D-glucose and 3 mM MgCl2, Kii Trypanosoma cruzi
0.0028
-
2-(pyridin-4-yl)-1-hydroxyethane-1,1-bisphosphonate varied substrate is ATP, in the presence of 2 mM D-glucose and 3 mM MgCl2, Kis Trypanosoma cruzi
0.0033
-
2-(pyridin-4-yl)-1-hydroxyethane-1,1-bisphosphonate varied substrate is D-glucose, in the presence of 1 mM ATP and 3 mM MgCl2, Kis Trypanosoma cruzi
0.0043
-
2-(pyridin-4-yl)-1-hydroxyethane-1,1-bisphosphonate varied substrate is ATP, in the presence of 2 mM D-glucose and 3 mM MgCl2, Kii Trypanosoma cruzi
0.006
-
2-(pyridin-4-yl)-1-hydroxyethane-1,1-bisphosphonate varied substrate is D-glucose, in the presence of 1 mM ATP and 3 mM MgCl2, Kii Trypanosoma cruzi
22 83 [[(9-ethyl-9H-carbazol-3-yl)amino]methylene]bis(phosphonic acid) against ATP, Kii Trypanosoma cruzi
32.8
-
(2-pyridin-4-ylethane-1,1-diyl)bis(phosphonic acid) against ATP, Kis Trypanosoma cruzi
33.3
-
(2-pyridin-4-ylethane-1,1-diyl)bis(phosphonic acid) against D-glucose, Kis Trypanosoma cruzi
34.3
-
(2-pyridin-4-ylethane-1,1-diyl)bis(phosphonic acid) Kii Trypanosoma cruzi
36
-
(2-pyridin-4-ylethane-1,1-diyl)bis(phosphonic acid) against D-glucose, Kii Trypanosoma cruzi
2281
-
[[(9-ethyl-9H-carbazol-3-yl)amino]methylene]bis(phosphonic acid) against D-glucose, Kis Trypanosoma cruzi
2282
-
[[(9-ethyl-9H-carbazol-3-yl)amino]methylene]bis(phosphonic acid) against ATP, Kis Trypanosoma cruzi
3020
-
[[(3-bromophenyl)amino]methylene]bis(phosphonic acid) against D-glucose, Kis Trypanosoma cruzi
3021
-
[[(3-bromophenyl)amino]methylene]bis(phosphonic acid) against ATP, Kii Trypanosoma cruzi
3021
-
[[(3-bromophenyl)amino]methylene]bis(phosphonic acid) against ATP, Kis Trypanosoma cruzi