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Literature summary for 2.5.1.21 extracted from

  • Sealey-Cardona, M.; Cammerer, S.; Jones, S.; Ruiz-Perez, L.M.; Brun, R.; Gilbert, I.H.; Urbina, J.A.; Gonzalez-Pacanowska, D.
    Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives (2007), Antimicrob. Agents Chemother., 51, 2123-2129.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.21

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli, several truncated versions of SQS with a His tag attached to the amino terminus Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
(3R)-3-[[3-(benzyloxy)phenyl]ethynyl]-1-azabicyclo[2.2.2]octan-3-ol IC50: 1500 nM Trypanosoma cruzi
3-(biphenyl-4-ylmethyl)-1-azabicyclo[2.2.2]oct-2-ene IC50: 730 nM Trypanosoma cruzi
3-[[4-(benzyloxy)phenyl]ethynyl]-1-azabicyclo[2.2.2]oct-2-ene IC50: 830 nM Trypanosoma cruzi
E5700 IC50: 0.84 nM Trypanosoma cruzi
ER119884 IC50: 3.52 nM Trypanosoma cruzi
ethyl 4-(1-azabicyclo[2.2.2]oct-2-en-3-yl)benzoate IC50: 50 nM Trypanosoma cruzi

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00525
-
 farnesyl diphosphate in 50 mM morpholinepropanesulfonic acid-NaOH buffer (pH 7.4), 20 mM MgCl2, 5 mM 3-[(3-cholamidopropyl)-dimethylammonio]-1-propanesulfonate, 1% Tween 80, 10 mM dithiothreitol, 0.025 mg/ml bovine serum albumin, 0.25 mM NADPH, at 37°C Trypanosoma cruzi
0.02334
-
 NADPH in 50 mM morpholinepropanesulfonic acid-NaOH buffer (pH 7.4), 20 mM MgCl2, 5 mM 3-[(3-cholamidopropyl)-dimethylammonio]-1-propanesulfonate, 1% Tween 80, 10 mM dithiothreitol, 0.025 mg/ml bovine serum albumin, 0.25 mM NADPH, at 37°C Trypanosoma cruzi

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
41670
-
 SDS-PAGE, estimated molecular mass Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Purification (Commentary)

Purification (Comment) Organism
HiTrap nickel-chelating column chromatography and MonoQ HR5/5 anion-exchange column chromatography Trypanosoma cruzi

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.1
-
 truncated protein, soluble extract Trypanosoma cruzi
0.459
-
 truncated protein, after 4.5fold purification Trypanosoma cruzi

Storage Stability

Storage Stability Organism
-80°C, 25 mM sodium phosphate (pH 7.4, containing 20 mM NaCl, 2 mM dithiothreitol, 1 mM EDTA, 40% glycerol, 10% methanol, 1 mM phenylmethylsulfonyl fluoride, 0.01 mM leupeptin, 0.001 mM pepstatin), extended periods of time, no loss of activity Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + NAD(P)H + H+
-
 Trypanosoma cruzi squalene + diphosphate + NAD(P)+
-
 ?

Synonyms

Synonyms Comment Organism
farnesyl-diphosphate farnesyltransferase
-
 Trypanosoma cruzi
SQS
-
 Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000084
-
 IC50: 0.84 nM Trypanosoma cruzi E5700
0.00000352
-
 IC50: 3.52 nM Trypanosoma cruzi ER119884
0.00005
-
 IC50: 50 nM Trypanosoma cruzi ethyl 4-(1-azabicyclo[2.2.2]oct-2-en-3-yl)benzoate
0.00073
-
 IC50: 730 nM Trypanosoma cruzi 3-(biphenyl-4-ylmethyl)-1-azabicyclo[2.2.2]oct-2-ene
0.00083
-
 IC50: 830 nM Trypanosoma cruzi 3-[[4-(benzyloxy)phenyl]ethynyl]-1-azabicyclo[2.2.2]oct-2-ene
0.0015
-
 IC50: 1500 nM Trypanosoma cruzi (3R)-3-[[3-(benzyloxy)phenyl]ethynyl]-1-azabicyclo[2.2.2]octan-3-ol