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Literature summary 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

Inhibitors

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

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.10 Trypanosoma cruzi
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.5.1.10 amastigote
-
Trypanosoma cruzi
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.5.1.10 farnesyl diphosphate synthase
-
Trypanosoma cruzi
2.5.1.10 FPPS
-
Trypanosoma cruzi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.10 0.0000027
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Mn(II)(risedronate)2]
2.5.1.10 0.0000029
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Ni(II)(risedronate)2]
2.5.1.10 0.000026
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi [Cu(II)(risedronate)2]
2.5.1.10 0.000027
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi risedronate
2.5.1.10 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
2.5.1.10 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]
2.5.1.10 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]
2.5.1.10 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]
2.5.1.10 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]
2.5.1.10 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]
2.5.1.10 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]
2.5.1.10 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]
2.5.1.10 0.00134
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi pamidronate
2.5.1.10 0.0044
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi alendronate
2.5.1.10 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]