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Literature summary for 2.5.1.10 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
Search for more literature for 2.5.1.10

Cloned(Commentary)

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

Crystallization (Commentary)

Crystallization (Comment) Organism
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

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Purification (Commentary)

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