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Literature summary extracted from

  • Aripirala, S.; Szajnman, S.H.; Jakoncic, J.; Rodriguez, J.B.; Docampo, R.; Gabelli, S.B.; Amzel, L.M.
    Design, synthesis, calorimetry, and crystallographic analysis of 2-alkylaminoethyl-1,1-bisphosphonates as inhibitors of Trypanosoma cruzi farnesyl diphosphate synthase (2012), J. Med. Chem., 55, 6445-6454.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.10 expressed in Escherichia coli BL21(DE3) cells Trypanosoma cruzi

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.5.1.10 in complex with Mg2+ and inhibitors, vapor diffusion method, using 100 mM sodium acetate, pH 4.6-5.2, 200 mM ammonium sulfate, and 2-10% (w/v) PEG 4K Trypanosoma cruzi

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.10 (2-[[(2E)-2,6-dimethylhepta-2,5-dien-1-yl]amino]ethane-1,1-diyl)bis(phosphonic acid)
-
 Trypanosoma cruzi
2.5.1.10 alendronate
-
 Trypanosoma cruzi
2.5.1.10 ibandronate
-
 Trypanosoma cruzi
2.5.1.10 pamidronate
-
 Trypanosoma cruzi
2.5.1.10 risedronate
-
 Trypanosoma cruzi
2.5.1.10 [2-(cyclohexylamino)ethane-1,1-diyl]bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 [2-(n-heptylamino)ethane-1,1-diyl]bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 [2-(n-hexylamino)ethane-1,1-diyl]bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 [2-(n-pentylamino)ethane-1,1-diyl]bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 [2-(npropylamino)ethane-1,1-diyl]bisphosphonic acid
-
 Trypanosoma cruzi
2.5.1.10 [2-[(2-methylprop-2-en-1-yl)amino]ethane-1,1-diyl]bis(phosphonic acid)
-
 Trypanosoma cruzi

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.5.1.10 Mg2+ required Trypanosoma cruzi

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.10 HisTrap Ni2+ chelate affinity chromatography 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 0.000038
-
 pH and temperature not specified in the publication Trypanosoma cruzi [2-(npropylamino)ethane-1,1-diyl]bisphosphonic acid
2.5.1.10 0.000058
-
 pH and temperature not specified in the publication Trypanosoma cruzi [2-(n-heptylamino)ethane-1,1-diyl]bisphosphonic acid
2.5.1.10 0.00049
-
 pH and temperature not specified in the publication Trypanosoma cruzi [2-(n-hexylamino)ethane-1,1-diyl]bisphosphonic acid
2.5.1.10 0.00184
-
 pH and temperature not specified in the publication Trypanosoma cruzi [2-(n-pentylamino)ethane-1,1-diyl]bisphosphonic acid