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Literature summary for 4.1.1.50 extracted from

  • Beswick, T.C.; Willert, E.K.; Phillips, M.A.
    Mechanisms of allosteric regulation of Trypanosoma cruzi S-adenosylmethionine decarboxylase (2006), Biochemistry, 45, 7797-7807.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
(2E)-2-[4-[amino(imino)methyl]-2,3-dihydro-1H-inden-1-ylidene]hydrazinecarboximidamide stimulation in the range of 0.1-10 microM, inhibition at higher comcentration Trypanosoma cruzi
putrescine stimulates ration kcat/Km for wild-type 27fold, also stimulates binding of inhibitors (2E)-2-[4-[amino(imino)methyl]-2,3-dihydro-1H-inden-1-ylidene]hydrazinecarboximidamide and 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide Trypanosoma cruzi

Protein Variants

Protein Variants Comment Organism
D174V residue in putrescine binding site, no activation by putrescine Trypanosoma cruzi
F285H residue in putrescine binding site, enhanced catalytic activity Trypanosoma cruzi
S111R residue in putrescine binding site, reduced catalytic activity Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
(2E)-2-[(2E)-2-[(diaminomethyl)hydrazono]-1-methylethylidene]hydrazinecarboximidamide i.e. MGBG, active site inhibitor Trypanosoma cruzi
(2E)-2-[4-[amino(imino)methyl]-2,3-dihydro-1H-inden-1-ylidene]hydrazinecarboximidamide i.e. CGP 48664A, stimulation in the range of 0.1-10 microM, inhibition at higher comcentration. Binds to the putrescine binding site and to the active site Trypanosoma cruzi
3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide i.e. CGP40215, active site inhibitor Trypanosoma cruzi

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information ratio of kcat/Km value, wild-type 3.5 per M and s in absence, 100 per M and s in presence of putrescine, mutant S111R 2.0 per M and s in absence, 6.4 per M and s in presence of putrescine, mutant D174V 36.6 per M and s in absence, 5 per M and s in presence of putrescine, mutant F285 1.8 per M and s in absence, 650 per M and s in presence of putrescine Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine
-
Trypanosoma cruzi (5-deoxy-5-adenosyl)(3-aminopropyl)methylsulfonium salt + CO2
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.2
-
mutant F285H, presence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
3.2
-
wild-type, presence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
13
-
mutant D174V, absence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
14
-
mutant D174V, presence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
26
-
mutant F285H, absence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
32
-
wild-type, absence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
96
-
mutant S111R, absence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide
104
-
mutant S111R, presence of putrescine, 37°C, pH 8.0 Trypanosoma cruzi 3-[(E)-[(2E)-[amino[(2E)-2-[3-[amino(imino)methyl]benzylidene]hydrazino]methylene]hydrazono]methyl]benzenecarboximidamide