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Literature summary extracted from

  • Rosso, V.S.; Szajnman, S.H.; Malayil, L.; Galizzi, M.; Moreno, S.N.; Docampo, R.; Rodriguez, J.B.
    Synthesis and biological evaluation of new 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase (2011), Bioorg. Med. Chem., 19, 2211-2217.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.5.1.10 medicine the enzyme is a target for Chagas’ disease chemotherapy Trypanosoma cruzi

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.10 1-[(benzylamino)ethyl] 1,1-bisphosphonic acid
-
 Toxoplasma gondii
2.5.1.10 1-[(benzylamino)ethyl] 1,1-bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 1-[(n-dec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Toxoplasma gondii
2.5.1.10 1-[(n-dec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 1-[(n-dodec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Toxoplasma gondii
2.5.1.10 1-[(n-dodec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 1-[(n-non-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Toxoplasma gondii
2.5.1.10 1-[(n-non-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 1-[(n-tetradec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Toxoplasma gondii
2.5.1.10 1-[(n-tetradec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 1-[(n-undec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Toxoplasma gondii
2.5.1.10 1-[(n-undec-1-ylamino)ethyl] 1,1-bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 alendronate
-
 Toxoplasma gondii
2.5.1.10 alendronate
-
 Trypanosoma cruzi
2.5.1.10 ibandronate
-
 Toxoplasma gondii
2.5.1.10 ibandronate
-
 Trypanosoma cruzi
2.5.1.10 pamidronate
-
 Toxoplasma gondii
2.5.1.10 pamidronate
-
 Trypanosoma cruzi
2.5.1.10 risedronate
-
 Toxoplasma gondii
2.5.1.10 risedronate
-
 Trypanosoma cruzi
2.5.1.10 [2-(heptylamino)ethane-1,1-diyl]bis(phosphonic acid)
-
 Toxoplasma gondii
2.5.1.10 [2-(heptylamino)ethane-1,1-diyl]bis(phosphonic acid)
-
 Trypanosoma cruzi
2.5.1.10 [2-(hexylamino)ethane-1,1-diyl]bis(phosphonic acid) competitive inhibitor Toxoplasma gondii
2.5.1.10 [2-(hexylamino)ethane-1,1-diyl]bis(phosphonic acid) competitive inhibitor Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.10 Toxoplasma gondii Q197X6
-
-
2.5.1.10 Trypanosoma cruzi
-
-
-

Source Tissue

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

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
-
 ?
2.5.1.10 geranyl diphosphate + isopentenyl diphosphate
-
 Toxoplasma gondii diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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 0.000058
-
 pH and temperature not specified in the publication Trypanosoma cruzi [2-(heptylamino)ethane-1,1-diyl]bis(phosphonic acid)
2.5.1.10 0.000068
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii 1-[(n-dec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.000074
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii risedronate
2.5.1.10 0.000093
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii 1-[(n-dodec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.00014
-
 pH and temperature not specified in the publication Toxoplasma gondii [2-(hexylamino)ethane-1,1-diyl]bis(phosphonic acid)
2.5.1.10 0.000292
-
 IC50 above 0.001 mM, in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii 1-[(n-tetradec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.00043
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi 1-[(n-non-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.00044
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii 1-[(n-non-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.000811
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi 1-[(n-dodec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.000856
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi 1-[(n-undec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.000868
-
 in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii 1-[(n-undec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.001
-
 IC50 above 0.001 mM, in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi 1-[(n-dec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.001
-
 IC50 above 0.001 mM, in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi 1-[(n-tetradec-1-ylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.001
-
 IC50 above 0.001 mM, in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi 1-[(benzylamino)ethyl] 1,1-bisphosphonic acid
2.5.1.10 0.00135
-
 pH and temperature not specified in the publication Trypanosoma cruzi [2-(hexylamino)ethane-1,1-diyl]bis(phosphonic acid)