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Literature summary 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

EC Number Inhibitors Comment Organism Structure
2.4.2.8 (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
2.4.2.8 [(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

EC Number Organism UniProt Comment Textmining
2.4.2.8 Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.4.2.8 HGXPRT
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.2.8 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
2.4.2.8 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