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Literature summary for 1.1.1.44 extracted from

  • Ruda, G.F.; Alibu, V.P.; Mitsos, C.; Bidet, O.; Kaiser, M.; Brun, R.; Barrett, M.P.; Gilbert, I.H.
    Synthesis and biological evaluation of phosphate prodrugs of 4-phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase (2007), ChemMedChem, 2, 1169-1180.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
4-phospho-D-erythronohydroxamic acid conversion of the 6-PGDH inhibitor into prodrugs to increase its activity against the Trypanosoma brucei by enhancing uptake by passive permeation across the plasma membrane. Production of five different phosphate-masking groups (phosphoramidate, bis-S-acyl thioethyl esters, bis-pivaloxymethyl, cycloSaligenyl and phenyl, S-acyl thioethyl mixed phosphate esters). Prodrugs are studied for stability and activity against the intact parasites. Most prodrugs cause inhibition of the growth of the parasites. The activity of the prodrugs against the parasites appears to be related to their stability in aqueous buffer Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
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-
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Synonyms

Synonyms Comment Organism
6-PGDH
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Trypanosoma brucei
6-phosphogluconate dehydrogenase
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Trypanosoma brucei