Selective inhibition of Trypanosoma cruzi GAPDH by "bi-substrate" analogues.
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.
Ladame
Sylvain
S
University Chemical Laboratory, University of Cambridge, Cambridge CB2 1EW, UK. sl324@cam.ac.uk
Fauré
Régis
R
Denier
Colette
C
Lakhdar-Ghazal
Faouzi
F
Willson
Michèle
M
D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005987:Glyceraldehyde-3-Phosphate Dehydrogenases / Q000037:antagonists & inhibitors*; D014349:Trypanosoma cruzi / Q000201:enzymology*
D004791:Enzyme Inhibitors; D005987:Glyceraldehyde-3-Phosphate Dehydrogenases