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Theses

Synthèse d'analogues de l'acide glutamique par transamination enzymatique : Synthèse et Modélisation

Abstract : Glutamate (Glu) is the major excitatory neurotransmitter within the brain where numerous different specific receptors and transporters have been identified. Glu analogues can behave as selective ligands and are very important for elucidating the specific roles of these receptors. The object of this phd study was to prepare new functionalized Glu analogues using Aminotransférases as biocatalysts allowing the stereoselective conversion of 2- oxoglutaric analogues (KG) into Glu analogues. Many of these KG analogues proved to be good substrates of E.coli Aspartate Aminotransférase (AspAT) which allowed the stereoselective preparation of the corresponding Glu analogues. A modelling study has been performed to understand the AspAT substrate specificity. Four analogues displayed a high selectivity and offer today very interesting perspectives from the design of new drugs active in the glutamatergic system.
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Submitted on : Monday, July 16, 2012 - 5:25:11 PM
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  • HAL Id : tel-00718372, version 1

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Emmanuelle Sagot. Synthèse d'analogues de l'acide glutamique par transamination enzymatique : Synthèse et Modélisation. Chimie organique. Université Blaise Pascal - Clermont-Ferrand II, 2007. Français. ⟨NNT : 2007CLF21788⟩. ⟨tel-00718372⟩

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