| Autor: |
Dax, Chantal, Duffieux, Francis, Chabot, Nicolas, Coincon, Mathieu, Sygusch, Jurgen, A. M. Michels, Paul, Blonski, Casimir |
| Zdroj: |
Journal of Medicinal Chemistry; March 2006, Vol. 49 Issue: 5 p1499-1502, 4p |
| Abstrakt: |
An irreversible competitive inhibitor hydroxynaphthaldehyde phosphate was synthesized that is highly selective against the glycolytic enzyme fructose 1,6-bisphosphate aldolase from Trypanosoma brucei (causative agent of sleeping sickness). Inhibition involves Schiff base formation by the inhibitor aldehyde with Lys116 followed by reaction of the resultant Schiff base with a second residue. Molecular simulations indicate significantly greater molecular geometries conducive for nucleophilic attack in T. brucei aldolase than the mammalian isozyme and suggest Ser48 as the Schiff base modifying residue. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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