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Literature summary for 2.5.1.10 extracted from

  • Demoro, B.; Caruso, F.; Rossi, M.; Benitez, D.; Gonzalez, M.; Cerecetto, H.; Galizzi, M.; Malayil, L.; Docampo, R.; Faccio, R.; Mombru, A.W.; Gambino, D.; Otero, L.
    Bisphosphonate metal complexes as selective inhibitors of Trypanosoma cruzi farnesyl diphosphate synthase (2012), Dalton Trans., 41, 6468-6476.
    View publication on PubMed
Search for more literature for 2.5.1.10

Inhibitors

Inhibitors Comment Organism Structure
([Cu(II)(pamidronate)]H2O)n
-
 Trypanosoma cruzi
alendronate i.e. 4-amino-1-hydroxybutane-1,1-diylphosphonic acid Trypanosoma cruzi
pamidronate i.e. 3-amino-1-hydroxypropane-1,1-diylphosphonic acid Trypanosoma cruzi
risedronate i.e. 1-hydroxy-2-(pyridin-3-yl)ethane-1,1-diylphosphonic acid Trypanosoma cruzi
[Co(II)(pamidronate)2(H2O)2]
-
 Trypanosoma cruzi
[Co(II)(risedronate)2]
-
 Trypanosoma cruzi
[Co(II)2(alendronate)4(H2O)2]
-
 Trypanosoma cruzi
[Cu(II)(risedronate)2]
-
 Trypanosoma cruzi
[Cu(II)2(alendronate)4(H2O)2]
-
 Trypanosoma cruzi
[Mn(II)(pamidronate)2(H2O)2]
-
 Trypanosoma cruzi
[Mn(II)(risedronate)2]
-
 Trypanosoma cruzi
[Mn(II)2(alendronate)4(H2O)2]
-
 Trypanosoma cruzi
[Ni(II)(pamidronate)2(H2O)2]
-
 Trypanosoma cruzi
[Ni(II)(risedronate)2]
-
 Trypanosoma cruzi
[Ni(II)2(alendronate)4(H2O)2]
-
 Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
amastigote
-
 Trypanosoma cruzi
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
geranyl diphosphate + isopentenyl diphosphate
-
 Trypanosoma cruzi diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
farnesyl diphosphate synthase
-
 Trypanosoma cruzi
FPPS
-
 Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000027
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Mn(II)(risedronate)2]
0.0000029
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Ni(II)(risedronate)2]
0.000026
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Cu(II)(risedronate)2]
0.000027
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi risedronate
0.000095
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi ([Cu(II)(pamidronate)]H2O)n
0.0001
-
 IC50 above 0.0001 mM, in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Co(II)(risedronate)2]
0.000128
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Mn(II)2(alendronate)4(H2O)2]
0.000161
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Mn(II)(pamidronate)2(H2O)2]
0.000167
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Ni(II)2(alendronate)4(H2O)2]
0.000215
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Co(II)(pamidronate)2(H2O)2]
0.000328
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Ni(II)(pamidronate)2(H2O)2]
0.000717
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Cu(II)2(alendronate)4(H2O)2]
0.00134
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi pamidronate
0.0044
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi alendronate
0.05
-
 IC50 above 0.05 mM, in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Co(II)2(alendronate)4(H2O)2]