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Literature summary for 7.6.2.2 extracted from

  • Lekostaj, J.K.; Amoah, L.E.; Roepe, P.D.
    A single S1034C mutation confers altered drug sensitivity to PfMDR1 ATPase activity that is characteristic of the 7G8 isoform (2008), Mol. Biochem. Parasitol., 157, 107-111.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Protein Variants

Protein Variants Comment Organism
D1246Y highest ATPase activity of all mutants tested Plasmodium falciparum
N1042D kinetics similar to wild-type Plasmodium falciparum
N1042D/D1246Y kinetics similar to wild-type Plasmodium falciparum
S1034C not sensitive to mefloquine Plasmodium falciparum
S1034C/D1246Y decrease in Km value for ATP, slightly less sensitive to vanadate than wild-type Plasmodium falciparum
S1034C/N1042D kinetics similar to wild-type, less sensitive to vanadate Plasmodium falciparum
S1034C/N1042D/D1246Y 3.5fold increase in Km value Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
mefloquine
-
 Plasmodium falciparum
vanadate
-
 Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.226
-
 ATP mutant S1034C/D1246Y, pH 7.5, 37°C Plasmodium falciparum
0.369
-
 ATP mutant N1042D, pH 7.5, 37°C Plasmodium falciparum
0.879
-
 ATP mutant D1246Y, pH 7.5, 37°C Plasmodium falciparum
1.82
-
 ATP mutant S1034C/N1042D, pH 7.5, 37°C Plasmodium falciparum
2.14
-
 ATP wild-type, pH 7.5, 37°C Plasmodium falciparum
2.78
-
 ATP mutant N1042D/D1246Y, pH 7.5, 37°C Plasmodium falciparum
5.53
-
 ATP mutant S1034C, pH 7.5, 37°C Plasmodium falciparum
8.15
-
 ATP mutant S1034C/N1042D/D1246Y, pH 7.5, 37°C Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
 isoform MDR1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + verapamil/in
-
 Plasmodium falciparum ADP + phosphate + verapamil/out
-
 ?

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7 7.5 wild-type and all mutants tested Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.25
-
 wild-type, pH 7.5, 37°C Plasmodium falciparum vanadate
3.65
-
 mutant S1034C/D1246Y, pH 7.5, 37°C Plasmodium falciparum vanadate
4.29
-
 mutant N1042D/D1246Y, pH 7.5, 37°C Plasmodium falciparum vanadate
4.36
-
 mutant D1246Y, pH 7.5, 37°C Plasmodium falciparum vanadate
4.36
-
 mutant S1034C, pH 7.5, 37°C Plasmodium falciparum vanadate
4.55
-
 mutant N1042D, pH 7.5, 37°C Plasmodium falciparum vanadate
7
-
 mutant S1034C/N1042D, pH 7.5, 37°C Plasmodium falciparum vanadate