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Literature summary for 7.2.2.3 extracted from

  • Rosling, J.E.O.; Ridgway, M.C.; Summers, R.L.; Kirk, K.; Lehane, A.M.
    Biochemical characterization and chemical inhibition of PfATP4-associated Na+-ATPase activity in Plasmodium falciparum membranes (2018), J. Biol. Chem., 293, 13327-13337 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.2.2.3

Protein Variants

Protein Variants Comment Organism
T418N the mutant shows a lower level of inhibition by cipargamin compared to the wild type enzyme Plasmodium falciparum
T418N/P990R the mutant shows a lower level of inhibition by cipargamin compared to the wild type enzyme Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
cipargamin previously known as KAE609 and NITD609, complete inhibition at 500 nM Plasmodium falciparum
MMV000642
-
 Plasmodium falciparum
MMV000648
-
 Plasmodium falciparum
MMV000653
-
 Plasmodium falciparum
MMV000662
-
 Plasmodium falciparum
MMV000917
-
 Plasmodium falciparum
MMV006427
-
 Plasmodium falciparum
MMV006429
-
 Plasmodium falciparum
MMV006656
-
 Plasmodium falciparum
MMV006764
-
 Plasmodium falciparum
MMV007275
-
 Plasmodium falciparum
MMV007617
-
 Plasmodium falciparum
MMV008455
-
 Plasmodium falciparum
MMV011567
-
 Plasmodium falciparum
MMV020660
-
 Plasmodium falciparum
MMV396715
-
 Plasmodium falciparum
MMV396719
-
 Plasmodium falciparum
MMV396749
-
 Plasmodium falciparum
MMV665796
-
 Plasmodium falciparum
MMV665800
-
 Plasmodium falciparum
MMV665803
-
 Plasmodium falciparum
MMV665805
-
 Plasmodium falciparum
MMV665826
-
 Plasmodium falciparum
MMV665878
-
 Plasmodium falciparum
MMV665890
-
 Plasmodium falciparum
MMV665918
-
 Plasmodium falciparum
MMV665949
-
 Plasmodium falciparum
MMV666025
-
 Plasmodium falciparum
MMV666124
-
 Plasmodium falciparum
additional information not inhibited by MMV007839 and MMV000972 Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.23
-
 ATP at pH 7.2, temperature not specified in the publication Plasmodium falciparum
16.1
-
 Na+[side 1] at pH 7.2, temperature not specified in the publication Plasmodium falciparum

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + Na+[side 1] Plasmodium falciparum
-
 ADP + phosphate + Na+[side 2]
-
 ?
ATP + H2O + Na+[side 1] Plasmodium falciparum Dd2
-
 ADP + phosphate + Na+[side 2]
-
 ?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-
Plasmodium falciparum Dd2
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
 Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + Na+[side 1]
-
 Plasmodium falciparum ADP + phosphate + Na+[side 2]
-
 ?
ATP + H2O + Na+[side 1]
-
 Plasmodium falciparum Dd2 ADP + phosphate + Na+[side 2]
-
 ?

Synonyms

Synonyms Comment Organism
ATP4
-
 Plasmodium falciparum
Na+-ATPase
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
12.3
-
 wild type enzyme, at pH 7.2, temperature not specified in the publication Plasmodium falciparum cipargamin
21.1
-
 mutant enzyme T418N, at pH 7.2, temperature not specified in the publication Plasmodium falciparum cipargamin
32.5
-
 mutant enzyme T418N/P990R, at pH 7.2, temperature not specified in the publication Plasmodium falciparum cipargamin