Mabiala-Bassiloua, Charles-Gabin
Arthus-Cartier, Guillaume
Hannaert, Véronique
[UCL]
Thérisod, Hélène
Sygusch, Jurgen
Thérisod, Michel
Several 5-O-alkyl- and 5-C-alkyl-mannitol bis-phosphates were synthesized and comparatively assayed as inhibitors of fructose bis-phosphate aldolases (Fbas) from rabbit muscle (taken as surrogate model of the human enzyme) and from Trypanosoma brucei. A limited selectivity was found in several instances. Crystallographic studies confirm that the 5-O-methyl derivative binds competitively with substrate and the 5-O-methyl moiety penetrating deeper into a shallow hydrophobic pocket at the active site. This observation can lead to the preparation of selective competitive or irreversible inhibitors of the parasite Fba. © 2011 American Chemical Society.
Bibliographic reference |
Mabiala-Bassiloua, Charles-Gabin ; Arthus-Cartier, Guillaume ; Hannaert, Véronique ; Thérisod, Hélène ; Sygusch, Jurgen ; et. al. Mannitol bis-phosphate based inhibitors of fructose 1,6-bisphosphate aldolases. In: ACS Medicinal Chemistry Letters, Vol. 2, no. 11, p. 804-808 (2011) |
Permanent URL |
http://hdl.handle.net/2078.1/163568 |