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Literature summary for 2.7.11.12 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

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

Application

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(Commentary)

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

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 [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

Metals/Ions Comment Organism Structure
Mg2+
-
Plasmodium falciparum

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

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 [micromol/min/mg]

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 and Products (Substrate)

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

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
ATP
-
Plasmodium falciparum

IC50 Value

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