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Literature summary for 2.7.11.12 extracted from

  • Wiersma, H.I.; Galuska, S.E.; Tomley, F.M.; Sibley, L.D.; Liberator, P.A.; Donald, R.G.
    A role for coccidian cGMP-dependent protein kinase in motility and invasion (2004), Int. J. Parasitol., 34, 369-380.
    View publication on PubMed
Search for more literature for 2.7.11.12

Application

Application Comment Organism
pharmacology the enzyme is a target for coccidiostat pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine Eimeria tenella
pharmacology the enzyme is a target for coccidiostat pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine Toxoplasma gondii

Protein Variants

Protein Variants Comment Organism
additional information constructed PKG-knockout mutant parasite strains are refractory to to inhibitor pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine with reduced sensitivity, complementation by expression of Eimeria tenella PKG Toxoplasma gondii
additional information constructed PKG-knockout mutant parasite strains are refractory to to inhibitor pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine with reduced sensitivity, complementation by expression of Toxoplasma gondii PKG Eimeria tenella
T761M site-directed mutagenesis, mutant enzyme is not inhibited by pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine Toxoplasma gondii
T761Q site-directed mutagenesis, mutant enzyme is not inhibited by pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine Toxoplasma gondii
T770M site-directed mutagenesis, mutant enzyme is not inhibited by pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine Eimeria tenella
T770Q site-directed mutagenesis, mutant enzyme is not inhibited by pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine Eimeria tenella

Inhibitors

Inhibitors Comment Organism Structure
4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine inhibits downstream of calcium-dependent events, inhibition is not reversible by calcium ionophores or ethanol, inhibits uracil uptake, blocks the attachment of the sporozoite to the host cells and inhibits parasite invasion and gliding motility, inhibits the secretion of micronemal adhesins MIC1 and MIC2 by the parasite, no inhibition of mutants T770M and T770Q Eimeria tenella
4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine inhibits downstream of calcium-dependent events, inhibition is not reversible by calcium ionophores or ethanol, inhibits uracil uptake, blocks the attachment of the tachyzoite to the host cells and inhibits parasite invasion and gliding motility, inhibits the secretion of micronemal adhesin MIC2 by the parasite, no inhibition of mutants T761M and T761Q Toxoplasma gondii

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Eimeria tenella the enzyme is involved in coccidian parasite motility and invasion and is important in host-parasite interaction ?
-
 ?
additional information Toxoplasma gondii the enzyme is involved in coccidian parasite motility and invasion and is important in host-parasite interaction ?
-
 ?

Organism

Organism UniProt Comment Textmining
Eimeria tenella
-
 propagated in MDBK cells
-
Toxoplasma gondii
-
 propagated in MDBK cells
-

Source Tissue

Source Tissue Comment Organism Textmining
sporozoite
-
 Eimeria tenella
-
tachyzoite
-
 Toxoplasma gondii
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
 Eimeria tenella
additional information
-
-
 Toxoplasma gondii

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme is involved in coccidian parasite motility and invasion and is important in host-parasite interaction Eimeria tenella ?
-
 ?
additional information the enzyme is involved in coccidian parasite motility and invasion and is important in host-parasite interaction Toxoplasma gondii ?
-
 ?

Synonyms

Synonyms Comment Organism
PKG
-
 Eimeria tenella
PKG
-
 Toxoplasma gondii

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information
-
 Eimeria tenella
additional information
-
 additional information
-
 Toxoplasma gondii