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Literature summary for 2.5.1.10 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

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Toxoplasma gondii Q197X6
-
-
Trypanosoma cruzi
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000027
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Trypanosoma cruzi risedronate
0.000058
-
pH and temperature not specified in the publication Trypanosoma cruzi [2-(heptylamino)ethane-1,1-diyl]bis(phosphonic acid)
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
0.000074
-
in 10 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM dithiothreitol, at 37°C Toxoplasma gondii risedronate
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
0.00014
-
pH and temperature not specified in the publication Toxoplasma gondii [2-(hexylamino)ethane-1,1-diyl]bis(phosphonic acid)
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
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
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
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
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
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
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
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
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
0.00135
-
pH and temperature not specified in the publication Trypanosoma cruzi [2-(hexylamino)ethane-1,1-diyl]bis(phosphonic acid)