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Literature summary for 2.4.2.1 extracted from

  • Madrid, D.C.; Ting, L.M.; Waller, K.L.; Schramm, V.L.; Kim, K.
    Plasmodium falciparum purine nucleoside phosphorylase is critical for viability of malaria parasites (2008), J. Biol. Chem., 283, 35899-35907.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.2.1

Protein Variants

Protein Variants Comment Organism
additional information targeted gene disruption results in loss of enzyme activity in lysate, with normal activity of adenosine deaminase. Mutant parasites show a greater requirement for exogenous purines and a severe growth defect at physiological concentrations of hypoxanthine. The mutant parasites are more sensitive to purine nucelotide phosphorylase inhibitors that bind human purine nucelotide phosphorylase tighter and less sensitive to inhibitor 5'-methylthio-immucillin-H Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
2'-deoxy-immucillin-G
-
 Plasmodium falciparum
2'-deoxy-immucillin-H
-
 Plasmodium falciparum
5'-methylthio-immucillin-H
-
 Plasmodium falciparum
immucillin-H
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8T9Z7 3D7
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.016
-
 substrate 5'-methylthioinosine, pH 7.4 Plasmodium falciparum
0.023
-
 substrate inosine, pH 7.4 Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5'-methylthioinosine + phosphate
-
 Plasmodium falciparum hypoxanthine + 5-methylthio-alpha-D-ribose 1-phosphate
-
 ?
inosine + phosphate
-
 Plasmodium falciparum hypoxanthine + alpha-D-ribose 1-phosphate
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000064
-
 gene disruption mutant, pH 7.4 Plasmodium falciparum 2'-deoxy-immucillin-G
0.0000085
-
 gene disruption mutant, pH 7.4 Plasmodium falciparum immucillin-H
0.000016
-
 gene disruption mutant, pH 7.4 Plasmodium falciparum 2'-deoxy-immucillin-H
0.000043
-
 wild-type, pH 7.4 Plasmodium falciparum immucillin-H
0.000086
-
 wild-type, pH 7.4 Plasmodium falciparum 5'-methylthio-immucillin-H
0.00044
-
 wild-type, pH 7.4 Plasmodium falciparum 2'-deoxy-immucillin-H
0.00053
-
 wild-type, pH 7.4 Plasmodium falciparum 2'-deoxy-immucillin-G
0.0009
-
 gene disruption mutant, pH 7.4 Plasmodium falciparum 5'-methylthio-immucillin-H

General Information

General Information Comment Organism
physiological function targeted gene disruption results in loss of enzyme activity in lysate, with normal activity of adenosine deaminase. Mutant parasites show a greater requirement for exogenous purines and a severe growth defect at physiological concentrations of hypoxanthine. The mutant parasites are more sensitive to purine nucleoside phosphorylase inhibitors that bind human purine nucelotide phosphorylase tighter and less sensitive to inhibitor 5'-methylthio-immucillin-H Plasmodium falciparum