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 | 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 | 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 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 | UniProt | Comment | Textmining |
---|---|---|---|
Trypanosoma cruzi | - |
- |
- |
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 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 |