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Synthetic and crystallographic insight into exploiting sp2-hybridization in the development of α-L-fucosidase inhibitors

DOI: 10.1002/cbic.201800710 DOI Help

Authors: Travis Coyle (University of Western Australia) , Liang Wu (The University of York) , Aleksandra Debowski (University of Western Australia) , Gideon Davies (The University of York) , Keith A. Stubbs (University of Western Australia)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Chembiochem

State: Published (Approved)
Published: January 2019
Diamond Proposal Number(s): 18598

Open Access Open Access

Abstract: 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.

Journal Keywords: Enzyme Inhibitors; Fucosidases; glycosidases; hydroximolactone; carbamate

Diamond Keywords: Enzymes

Subject Areas: Biology and Bio-materials, Chemistry

Instruments: I03-Macromolecular Crystallography

Added On: 29/01/2019 11:35


Discipline Tags:

Biochemistry Chemistry Structural biology Life Sciences & Biotech

Technical Tags:

Diffraction Macromolecular Crystallography (MX)