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Synthetic and Crystallographic Insight into Exploiting sp2 Hybridization in the Development of ?-l-Fucosidase Inhibitors.

ABSTRACT: The sugar fucose plays a myriad of roles in biological recognition. Enzymes hydrolyzing fucose from glycoconjugates, ?-l-fucosidases, are important targets for inhibitor and probe development. Here we describe the synthesis and evaluation of novel ?-l-fucosidase inhibitors, with X-ray crystallographic analysis using an ?-l-fucosidase from Bacteroides thetaiotamicron helping to lay a foundation for future development of inhibitors for this important enzyme class.

SUBMITTER: Coyle T

PROVIDER: S-EPMC6589914 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Synthetic and Crystallographic Insight into Exploiting sp2 Hybridization in the Development of α-l-Fucosidase Inhibitors.

Coyle Travis T Wu Liang L Debowski Aleksandra W AW Davies Gideon J GJ Stubbs Keith A KA

Chembiochem : a European journal of chemical biology 20190318 11

The sugar fucose plays a myriad of roles in biological recognition. Enzymes hydrolyzing fucose from glycoconjugates, α-l-fucosidases, are important targets for inhibitor and probe development. Here we describe the synthesis and evaluation of novel α-l-fucosidase inhibitors, with X-ray crystallographic analysis using an α-l-fucosidase from Bacteroides thetaiotamicron helping to lay a foundation for future development of inhibitors for this important enzyme class. ...[more]

PMID: 30663832

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