Activating Compound | Comment | Organism | Structure |
---|---|---|---|
cGMP | cooperative kinetics of stimulation | Plasmodium falciparum |
Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a target for antiparasitic drugs, e.g. pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | Plasmodium falciparum |
Cloned (Comment) | Organism |
---|---|
DNA and amino acid sequence determination and analysis, transient expression of FLAG-tagged enzyme in Toxoplasma gondii parasites, comparison of properties of the recombinant enzyme to the native one | Plasmodium falciparum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | inhibits native and recombinant enzyme, shows antiparasitic activity being active against Plasmodium falciparum blood cell stages cultured in vitro, IC50 for the native enzyme is 8.35 nM, and for the recombinant FLAG-tagged enzyme 3.48 nM | Plasmodium falciparum |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | kinetics | Plasmodium falciparum | |
0.062 | - |
GRTGRRNSI | pH 7.4, 37°C, recombinant FLAG-tagged enzyme | Plasmodium falciparum |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Plasmodium falciparum |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
98000 | - |
x * 98000, native enzyme, SDS-PAGE | Plasmodium falciparum |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium falciparum | - |
- |
- |
Purification (Comment) | Organism |
---|---|
native enzyme is purified partially by cGMP affnity and ion exchange chromatography, recombinant FLAG-tagged enzyme from Toxoplasma gondii by anti-FLAG affinity chromatography | Plasmodium falciparum |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
0.000006 | - |
purified recombinant FLAG-tagged enzyme, substrate Glasstide | Plasmodium falciparum |
0.000028 | - |
purified recombinant FLAG-tagged enzyme, substrate Kemptide | Plasmodium falciparum |
0.000037 | - |
purified recombinant FLAG-tagged enzyme, substrate MCPD-4 | Plasmodium falciparum |
0.000041 | - |
purified recombinant FLAG-tagged enzyme, substrate histone H2B | Plasmodium falciparum |
0.0004 | - |
purified recombinant FLAG-tagged enzyme, substrate PKI | Plasmodium falciparum |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Arg-Lys-Arg-Ser-Arg-Ala-Glu | i.e. Glasstide, a commercial peptide substrate | Plasmodium falciparum | ADP + Arg-Lys-Arg-O-phospho-Ser-Arg-Ala-Glu | - |
? | |
ATP + GKKRKRSRKES | i.e. MCPD-4, a commercial peptide substrate | Plasmodium falciparum | ADP + GKKRKRS(P)RKES | - |
? | |
ATP + GRTGRRNSI | i.e. PKI, a commercial peptide substrate | Plasmodium falciparum | ADP + phosphorylated GRTGRRNSI | - |
? | |
ATP + histone H2B | - |
Plasmodium falciparum | ADP + phosphorylated histone H2B | - |
? | |
ATP + Kemptide | i.e. LRRASLG, a commercial peptide substrate | Plasmodium falciparum | ADP + phosphorylated Kemptide | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 98000, native enzyme, SDS-PAGE | Plasmodium falciparum |
Synonyms | Comment | Organism |
---|---|---|
cyclic GMP-dependent protein kinase | - |
Plasmodium falciparum |
PKG | - |
Plasmodium falciparum |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Plasmodium falciparum |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Plasmodium falciparum |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Plasmodium falciparum |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000348 | - |
IC50 for the recombinant FLAG-tagged enzyme 3.48 nM | Plasmodium falciparum | pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine | |
0.00000835 | - |
inhibits native and recombinant enzyme, shows antiparasitic activity being active against Plasmodium falsiparum blood cell stages cultured in vitro, IC50 for the native enzyme is 8.35 nM | Plasmodium falciparum | pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine |