Selective inhibition of Trypanosoma cruzi GAPDH by “bi-substrate” analogues

Sylvain Ladame (1, 2) , Régis Fauré (2) , Colette Denier (2) , Faouzi Lakhdar-Ghazal (2) , Michèle Willson (2)

1 Department of Chemical Engineering - University of Cambridge
2 SPCMIB - Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique

A new series of “bi-substrate” analogues have been synthesized as potential inhibitors of the glyceraldehyde-3-phosphate dehydrogenase and one lead compound has been identified that inhibits the enzyme from Trypanosoma cruzi with good affinity and very high (50-fold) specificity.

Domaines: Biochimie, Biologie Moléculaire

Sylvain Ladame, Régis Fauré, Colette Denier, Faouzi Lakhdar-Ghazal, Michèle Willson. Selective inhibition of Trypanosoma cruzi GAPDH by “bi-substrate” analogues. Organic & Biomolecular Chemistry, 2005, 3 (11), pp.2070. ⟨10.1039/B504703J⟩. ⟨hal-02146253⟩