Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli | Plasmodium falciparum |
Protein Variants | Comment | Organism |
---|---|---|
T618M | the amino acid substitution does not confer insensitivity to 4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | Plasmodium falciparum |
T618Q | mutant is over 3000fold less sensitive to 4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine and shows 10-20fold lower sensitivity to 4-[7-[(dimethylamino)methyl]-2-(4-fluorophenyl)imidazo[1,2-a]pyridine-3-yl]pyrimidin-2-amine than the wild type enzyme | Plasmodium falciparum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | highly specific ATP-competitive inhibitor of PKG | Plasmodium falciparum | |
4-[7-[(dimethylamino)methyl]-2-(4-fluorophenyl)imidazo[1,2-a]pyridine-3-yl]pyrimidin-2-amine | - |
Plasmodium falciparum |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Kemptide | Plasmodium falciparum | - |
ADP + Kemptide phosphate | - |
? | |
additional information | Plasmodium falciparum | PKG is essential for xanthurenic acid- and zaprinast-induced gametogenesis in Plasmodium falciparum | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium falciparum | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Plasmodium falciparum |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
gametocyte | - |
Plasmodium falciparum | - |
schizont | - |
Plasmodium falciparum | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Kemptide | - |
Plasmodium falciparum | ADP + Kemptide phosphate | - |
? | |
additional information | PKG is essential for xanthurenic acid- and zaprinast-induced gametogenesis in Plasmodium falciparum | Plasmodium falciparum | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PKG | - |
Plasmodium falciparum |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Plasmodium falciparum | |
cGMP | dependent | Plasmodium falciparum |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000155 | - |
mutant enzyme T618M, in 50 mM HEPES, at pH 7.4, at 30°C | Plasmodium falciparum | 4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | |
0.00000579 | - |
wild type enzyme, in 50 mM HEPES, at pH 7.4, at 30°C | Plasmodium falciparum | 4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | |
0.0178 | - |
mutant enzyme T618Q, in 50 mM HEPES, at pH 7.4, at 30°C | Plasmodium falciparum | 4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine |