Mannitol bis-phosphate based inhibitors of fructose 1,6-bisphosphate aldolases
(2011) ACS Medicinal Chemistry Letters — Vol. 2, n° 11, p. 804-808 (2011)
Files
pdfdocument.pdf
Restricted Access - Adobe PDF
- 827.21 KB
Details
- Authors
- Abstract
- 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.
- Affiliations
Citations
Mabiala-Bassiloua, C.-G., Arthus-Cartier, G., Hannaert, V., Thérisod, H., Sygusch, J., & Thérisod, M. (2011). Mannitol bis-phosphate based inhibitors of fructose 1,6-bisphosphate aldolases. ACS Medicinal Chemistry Letters, 2(11), 804-808. https://doi.org/10.1021/ml200129s (Original work published 2011)