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Literature summary extracted from

  • Diaz, C.A.; Allocco, J.; Powles, M.A.; Yeung, L.; Donald, R.G.; Anderson, J.W.; Liberator, P.A.
    Characterization of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG): Antiparasitic activity of a PKG inhibitor (2006), Mol. Biochem. Parasitol., 146, 78-88.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.12 cGMP cooperative kinetics of stimulation Plasmodium falciparum

Application

EC Number Application Comment Organism
2.7.11.12 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(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.12 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

EC Number Inhibitors Comment Organism Structure
2.7.11.12 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]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.11.12 additional information
-
 additional information kinetics Plasmodium falciparum
2.7.11.12 0.062
-
 GRTGRRNSI pH 7.4, 37°C, recombinant FLAG-tagged enzyme Plasmodium falciparum

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.12 Mg2+
-
 Plasmodium falciparum

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.11.12 98000
-
 x * 98000, native enzyme, SDS-PAGE Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.12 Plasmodium falciparum
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.12 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 [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.7.11.12 0.000006
-
 purified recombinant FLAG-tagged enzyme, substrate Glasstide Plasmodium falciparum
2.7.11.12 0.000028
-
 purified recombinant FLAG-tagged enzyme, substrate Kemptide Plasmodium falciparum
2.7.11.12 0.000037
-
 purified recombinant FLAG-tagged enzyme, substrate MCPD-4 Plasmodium falciparum
2.7.11.12 0.000041
-
 purified recombinant FLAG-tagged enzyme, substrate histone H2B Plasmodium falciparum
2.7.11.12 0.0004
-
 purified recombinant FLAG-tagged enzyme, substrate PKI Plasmodium falciparum

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.12 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
-
 ?
2.7.11.12 ATP + GKKRKRSRKES i.e. MCPD-4, a commercial peptide substrate Plasmodium falciparum ADP + GKKRKRS(P)RKES
-
 ?
2.7.11.12 ATP + GRTGRRNSI i.e. PKI, a commercial peptide substrate Plasmodium falciparum ADP + phosphorylated GRTGRRNSI
-
 ?
2.7.11.12 ATP + histone H2B
-
 Plasmodium falciparum ADP + phosphorylated histone H2B
-
 ?
2.7.11.12 ATP + Kemptide i.e. LRRASLG, a commercial peptide substrate Plasmodium falciparum ADP + phosphorylated Kemptide
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.12 ? x * 98000, native enzyme, SDS-PAGE Plasmodium falciparum

Synonyms

EC Number Synonyms Comment Organism
2.7.11.12 cyclic GMP-dependent protein kinase
-
 Plasmodium falciparum
2.7.11.12 PKG
-
 Plasmodium falciparum

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.12 37
-
 assay at Plasmodium falciparum

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.12 7.4
-
 assay at Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.12 ATP
-
 Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.12 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
2.7.11.12 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