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Literature summary for 2.4.2.1 extracted from

  • Daddona, P.E.; Wiesmann, W.P.; Milhouse, W.; Chern, J.W.; Townsend, L.B.; Hershfield, M.S.; Webster, H.K.
    Expression of human malaria parasite purine nucleoside phosphorylase in host enzyme-deficient erythrocyte culture. Enzyme characterization and identification of novel inhibitors (1986), J. Biol. Chem., 261, 11667-11673.
    View publication on PubMed

Application

Application Comment Organism
medicine
-
Homo sapiens
medicine the enzyme inhibitors 8-amino-5'-deoxy-5'-chloroguanosine and 8-amino-9-benzylguanine may have some antimalarial potential by limiting hypoxanthine production in the parasite-infected erythrocyte Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
5'-chloro-5'-deoxy-8-aminoguanosine
-
Homo sapiens
5'-chloro-5'-deoxy-8-aminoguanosine
-
Plasmodium falciparum
8-amino-5'-deoxy-5'-chloroguanosine
-
Homo sapiens
8-amino-5'-deoxy-5'-chloroguanosine
-
Plasmodium falciparum
8-Amino-9-benzylguanine
-
Homo sapiens
8-Amino-9-benzylguanine
-
Plasmodium falciparum
8-aminoguanosine
-
Homo sapiens
8-aminoguanosine
-
Plasmodium falciparum
formycin B
-
Homo sapiens
formycin B
-
Plasmodium falciparum
additional information the enzyme inhibitors 8-amino-5'-deoxy-5'-chloroguanosine and 8-amino-9-benzylguanine may have some antimalarial potential by limiting hypoxanthine production in the parasite-infected erythrocyte Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.01
-
Inosine
-
Plasmodium falciparum
0.01
-
guanosine
-
Plasmodium falciparum
0.035
-
guanosine
-
Homo sapiens
0.038
-
deoxyguanosine
-
Homo sapiens
0.041
-
Inosine
-
Homo sapiens
0.057
-
deoxyguanosine
-
Plasmodium falciparum
0.43
-
phosphate
-
Homo sapiens
0.68
-
phosphate
-
Plasmodium falciparum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
147000
-
sucrose density gradient centrifugation Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
deoxyguanosine + phosphate
-
Homo sapiens guanine + alpha-D-deoxyribose 1-phosphate
-
?
deoxyguanosine + phosphate
-
Plasmodium falciparum guanine + alpha-D-deoxyribose 1-phosphate
-
?
guanosine + phosphate
-
Homo sapiens guanine + alpha-D-ribose 1-phosphate
-
?
guanosine + phosphate
-
Plasmodium falciparum guanine + alpha-D-ribose 1-phosphate
-
?
inosine + phosphate
-
Homo sapiens hypoxanthine + alpha-D-ribose 1-phosphate
-
?
inosine + phosphate
-
Plasmodium falciparum hypoxanthine + alpha-D-ribose 1-phosphate
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0002
-
8-Amino-9-benzylguanine
-
Homo sapiens
0.0004
-
5'-chloro-5'-deoxy-8-aminoguanosine
-
Homo sapiens
0.0011
-
formycin B
-
Plasmodium falciparum
0.007
-
8-aminoguanosine
-
Homo sapiens
0.008
-
8-Amino-9-benzylguanine
-
Plasmodium falciparum
0.012
-
5'-chloro-5'-deoxy-8-aminoguanosine
-
Plasmodium falciparum
0.013
-
8-aminoguanosine
-
Plasmodium falciparum
0.13
-
formycin B
-
Homo sapiens