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- W2121922160 endingPage "277" @default.
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- W2121922160 abstract "Abstract Mannostatin A is a potent inhibitor of the mannose‐trimming enzyme, Golgi α‐mannosidase II (GMII), which acts late in the N ‐glycan processing pathway. Inhibition of this enzyme provides a route to blocking the transformation‐associated changes in cancer cell surface oligosaccharide structures. Here, we report on the synthesis of new Mannostatin derivatives and analyze their binding in the active site of Drosophila GMII by X‐ray crystallography. The results indicate that the interaction with the backbone carbonyl of Arg876 is crucial to the high potency of the inhibitor—an effect enhanced by the hydrophobic interaction between the thiomethyl group and an aromatic pocket vicinal to the cleavage site. The various structures indicate that differences in the hydration of protein–ligand complexes are also important determinants of plasticity as well as selectivity of inhibitor binding." @default.
- W2121922160 created "2016-06-24" @default.
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- W2121922160 creator A5074180325 @default.
- W2121922160 creator A5085497684 @default.
- W2121922160 date "2009-01-15" @default.
- W2121922160 modified "2023-10-18" @default.
- W2121922160 title "The Molecular Basis of Inhibition of Golgi α-Mannosidase II by Mannostatin A" @default.
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- W2121922160 doi "https://doi.org/10.1002/cbic.200800538" @default.
- W2121922160 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3956299" @default.
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