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Literature summary extracted from

  • Wurtz, N.; Chapus, C.; Desplans, J.; Parzy, D.
    cAMP-dependent protein kinase from Plasmodium falciparum: an update (2011), Parasitology, 138, 1-25.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.11 6-benzyl-cAMP activator of PfPKA catalytic subunit Plasmodium falciparum
2.7.11.11 cAMP binding of 2 cAMP molecules to each regulatory subunit alters its affinity for the catalytic subunit, resulting in release of the active catalytic subunit Plasmodium falciparum

Application

EC Number Application Comment Organism
2.7.11.11 drug development the enzyme represents an attractive target for the development of anti-malarial drugs Plasmodium falciparum

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.11 gene pfpkac encoding the catalytic subunit, phylogenetic analysis Plasmodium falciparum
2.7.11.11 gene pfpkar encoding the regulatory subunit, phylogenetic analysis and sequence comparison Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.11 H89 inhibits PfPKA catalytic subunit activity in vitro, leads to parasite growth arrest and morphological alteration; inhibits PfPKA catalytic subunit activity in vitro, leads to parasite growth arrest and morphological alteration Plasmodium falciparum
2.7.11.11 imatinib competes for the ATP binding site; competes for the ATP binding site Plasmodium falciparum
2.7.11.11 protein kinase inhibitor PKI, a natural endogenous inhibitor; PKI, a natural endogenous inhibitor Plasmodium falciparum

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.11 cytosol
-
 Plasmodium falciparum 5829
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.11 Mg2+ required Plasmodium falciparum

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.11.11 42200
-
 alpha2beta2, 2 * 42200, about, catalytic subunit, + 2 * 50800, about, regulatory subunit, sequence calculation Plasmodium falciparum
2.7.11.11 50800
-
 alpha2beta2, 2 * 42200, about, catalytic subunit, + 2 * 50800, about, regulatory subunit, sequence calculation Plasmodium falciparum

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.11 additional information Plasmodium falciparum the PKA catalytic subunit a serine/threonine kinase, that can phosphorylate many substrates, such as additional protein kinases and transcription factors ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.11 Plasmodium falciparum Q7K6A0 catalytic subunit
-
2.7.11.11 Plasmodium falciparum Q7KQK0 regulatory subunit
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.11 additional information in cytosolic extracts of both the asexual and sexual stages of the parasite, catalytic and regulatory subunits of PfPKA are expressed weakly during the ring and trophozoite stages compared to the schizont stage, and pfpkac mRNA levels are lower in gametocytes and gametes Plasmodium falciparum
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.11 additional information the PKA catalytic subunit a serine/threonine kinase, that can phosphorylate many substrates, such as additional protein kinases and transcription factors Plasmodium falciparum ?
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.11 heterotetramer alpha2beta2, 2 * 42200, about, catalytic subunit, + 2 * 50800, about, regulatory subunit, sequence calculation Plasmodium falciparum
2.7.11.11 More structure comparison with mammalian enzymes, overview Plasmodium falciparum

Synonyms

EC Number Synonyms Comment Organism
2.7.11.11 cyclic AMP-dependent protein kinase
-
 Plasmodium falciparum
2.7.11.11 PKA
-
 Plasmodium falciparum
2.7.11.11 protein kinase A
-
 Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.11 ATP residues of the PfPKA catalytic subunit G40, G42, and G45 are involved in ATP fixation, E82 in ATP stabiization, D175 in orienting the phosphate of ATP Plasmodium falciparum

pI Value

EC Number Organism Comment pI Value Maximum pI Value
2.7.11.11 Plasmodium falciparum regulatory subunit, sequence calculation
-
 7.49
2.7.11.11 Plasmodium falciparum catalytic subunit, sequence calculation
-
 9.11

General Information

EC Number General Information Comment Organism
2.7.11.11 malfunction downregulation of gene pfpkac mRNA using gene silencing leads to morphological changes in schizont stages and cell cycle arrest, and is also associated with a compensatory decrease in pfpkar mRNA levels, suggesting a transcriptional self-regulation of the PfPKA signalling network Plasmodium falciparum
2.7.11.11 metabolism the cAMP/PfPKA signalling pathway is essential for parasite growth and survival, mechanism and regulation, model of cAMP/PKA signalling pathway in Plasmodium falciparum, and of signalling events including PfPKA catalytic subunit during the Plasmodium falciparum life cycle, overview. The cAMP pathway regulates sporozoite motility and hepatic cell invasion by Plasmodium falciparum sporozoites. Putative role for PfPKA in the induction of gametocytogenesis, in erythrocyte invasion by merozoites, and in the regulation of mitochondrial protein traffic. Highly complex relationship between cAMP/PfPKA and calcium pathways in the asexual life cycle, with a key role of PfPKA in anion transport across the erythrocyte membrane, overview Plasmodium falciparum
2.7.11.11 additional information PKA has two regulatory subunits, which bind to and inhibit two catalytic subunits, domain organization and structure comparison with mammalian/human enzymes, overview. Sequence E221-C226-P227-P228-F229-Y23 and residue E161 of the PfPKA catalytic subunit are involved in substrate recognition, residues K63, D211, D157, N162, and E199 are required for catalysis Plasmodium falciparum
2.7.11.11 physiological function Plasmodium falciparum cAMP-dependent protein kinase plays an important role in the parasite's life cycle. The parasites appear to have tightly controlled mechanisms for selfregulating PfPKA levels to maintain appropriate PKA signalling Plasmodium falciparum