Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.12 extracted from

  • McRobert, L.; Taylor, C.J.; Deng, W.; Fivelman, Q.L.; Cummings, R.M.; Polley, S.D.; Billker, O.; Baker, D.A.
    Gametogenesis in malaria parasites is mediated by the cGMP-dependent protein kinase (2008), PLoS Biol., 6, e139.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Plasmodium falciparum

Protein Variants

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

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Plasmodium falciparum

Source Tissue

Source Tissue Comment Organism Textmining
gametocyte
-
Plasmodium falciparum
-
schizont
-
Plasmodium falciparum
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
PKG
-
Plasmodium falciparum

Cofactor

Cofactor Comment Organism Structure
ATP
-
Plasmodium falciparum
cGMP dependent Plasmodium falciparum

IC50 Value

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