Exploiting sp(2) -Hybridisation in the Development of Potent 1,5-α-l-Arabinanase Inhibitors.
Identifieur interne : 000C51 ( Main/Exploration ); précédent : 000C50; suivant : 000C52Exploiting sp(2) -Hybridisation in the Development of Potent 1,5-α-l-Arabinanase Inhibitors.
Auteurs : Travis Coyle [Australie] ; Aleksandra W. Debowski [Australie] ; Annabelle Varrot [France] ; Keith A. Stubbs [Australie]Source :
- Chembiochem : a European journal of chemical biology [ 1439-7633 ] ; 2017.
Descripteurs français
- KwdFr :
- MESH :
- antagonistes et inhibiteurs : Glycosidases.
- synthèse chimique : Antienzymes, Réactifs chromogènes.
- Cristallographie aux rayons X, Fusarium, Modèles moléculaires, Relation structure-activité.
English descriptors
- KwdEn :
- MESH :
- chemical , antagonists & inhibitors : Glycoside Hydrolases.
- chemical , chemical synthesis : Chromogenic Compounds, Enzyme Inhibitors.
- chemistry : Fusarium.
- Crystallography, X-Ray, Models, Molecular, Structure-Activity Relationship.
Abstract
The synthesis of potent inhibitors of GH93 arabinanases as well as a synthesis of a chromogenic substrate to measure GH93 arabinanase activity are described. An insight into the reasons behind the potency of the inhibitors was gained through X-ray crystallographic analysis of the arabinanase Arb93A from Fusarium graminearum. These compounds lay a foundation for future inhibitor development as well as for the use of the chromogenic substrate in biochemical studies of GH93 arabinanases.
DOI: 10.1002/cbic.201700073
PubMed: 28266777
Affiliations:
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Le document en format XML
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