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Literature summary for 2.4.2.8 extracted from

  • Hazleton, K.Z.; Ho, M.C.; Cassera, M.B.; Clinch, K.; Crump, D.R.; Rosario, I.; Merino, E.F.; Almo, S.C.; Tyler, P.C.; Schramm, V.L.
    Acyclic immucillin phosphonates: second-generation inhibitors of Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase (2012), Chem. Biol., 19, 721-730.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(3-[[(4-oxo-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]amino]propyl)phosphonic acid competitive. 466fold lower affinity for human enzyme. Treatment of cultured parasites with the bis-pavalate of the inhibitor as a prodrug inhibits growth with an IC50 of 45 microM Plasmodium falciparum
[(3S)-4-hydroxy-3-[[(4-oxo-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]amino]butyl]phosphonic acid competitive. 592fold lower affinity for human enzyme Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
guanine + 5-phospho-alpha-D-ribose 1-diphosphate
-
Plasmodium falciparum GMP + diphosphate
-
?
xanthine + 5-phospho-alpha-D-ribose 1-diphosphate
-
Plasmodium falciparum XMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
HGXPRT
-
Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000065
-
[(3S)-4-hydroxy-3-[[(4-oxo-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]amino]butyl]phosphonic acid pH 7.6, 37°C Plasmodium falciparum
0.00001
-
(3-[[(4-oxo-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]amino]propyl)phosphonic acid pH 7.6, 37°C Plasmodium falciparum