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Literature summary for 3.1.4.35 extracted from

  • Yuasa, K.; Mi-Ichi, F.; Kobayashi, T.; Yamanouchi, M.; Kotera, J.; Kita, K.; Omori, K.
    PfPDE1, a novel cGMP-specific phosphodiesterase from the human malaria parasite Plasmodium falciparum (2005), Biochem. J., 392, 221-229.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.4.35

Application

Application Comment Organism
medicine the enzyme is suggested to be a potential target for the treatment of malaria Plasmodium falciparum

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Plasmodium falciparum

Protein Variants

Protein Variants Comment Organism
D762A mutant protein shows no cGMP hydrolytic activity Plasmodium falciparum
G788A mutant enzyme retains cGMP hydrolytic activity, KM-value is nearly identical to wild-type value, the IC50-value for zaprinast is 1.5fold higher than wild-type value Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
dipyridamole IC50: 0.022 mM Plasmodium falciparum
E4021 IC50: 0.046 mM Plasmodium falciparum
additional information 3-isobutyl-1-methylxanthine, theophylline and the antimalarial chloroquine show IC50-value of over 0.1 mM Plasmodium falciparum
sildenafil IC50: 0.056 mM Plasmodium falciparum
zaprinast IC50: 0.0038 mM for wild-type enzyme and 0.0056 for mutant enzyme G788A Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00065
-
 3',5'-cGMP wild-type enzyme Plasmodium falciparum
0.00077
-
 3',5'-cGMP mutant enzyme G788A Plasmodium falciparum

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Plasmodium falciparum 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ less active activator than Mn2+ Plasmodium falciparum
Mg2+ less active activator than Mn2+ Plasmodium falciparum
Mn2+ more potent activator of PfPDE1 than Mg2+ and Ca2+ at concentrations of 0.01-10 mM, maximal activity at 1 mM MnCl2 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q2V2M6
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cGMP + H2O specific for 3',5'-cGMP Plasmodium falciparum 5'-GMP
-
 ?

Synonyms

Synonyms Comment Organism
cGMP-specific phosphodiesterase
-
 Plasmodium falciparum
PfPDE1
-
 Plasmodium falciparum
xGMP-specific PDE
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0038
-
 IC50: 0.0038 mM for wild-type enzyme and 0.0056 for mutant enzyme G788A Plasmodium falciparum zaprinast
0.022
-
 IC50: 0.022 mM Plasmodium falciparum dipyridamole
0.046
-
 IC50: 0.046 mM Plasmodium falciparum E4021
0.056
-
 IC50: 0.056 mM Plasmodium falciparum sildenafil