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Preparation, biochemical characterization and biological properties of radiolabelled N-alkylated deoxynojirimycins.
TLDR
The reductively alkylated deoxynojirimycin imino sugars using sodium cyanoborotriti-ide to provide an efficient means of generating a series of N-alkylated compounds containing 4-18 carbon side chains are evaluated for their inhibitory effects on ceramide-specific glucosyltransferase and glycoprotein-processing alpha-glucosidase.
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Inhibition of alpha-L-fucosidase by derivatives of deoxyfuconojirimycin and deoxymannojirimycin.
TLDR
It is concluded that the minimum structural requirement for inhibition of alpha-L-fucosidase is the correct configuration of the hydroxy groups at the piperidine ring carbon atoms 2, 3 and 4.
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Glucose analogue inhibitors of glycogen phosphorylase: the design of potential drugs for diabetes.
TLDR
The kinetic and crystallographic studies have been combined to provide rationalizations for the apparent affinities of glucose and the analogues and show the discrimination against beta-D-glucose is achieved by an additional hydrogen bond made in the alpha- glucose complex through water to a protein group and an unfavorable environment for a polar group in the beta pocket.
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POTENT INHIBITION OF GLYCOGEN PHOSPHORYLASE BY A SPIROHYDANTOIN OF GLUCOPYRANOSE : FIRST PYRANOSE ANALOGUES OF HYDANTOCIDIN
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Glucose analogue inhibitors of glycogen phosphorylase: from crystallographic analysis to drug prediction using GRID force-field and GOLPE variable selection.
TLDR
The computational procedure described in this work involves the use of the program GRID to describe the molecular structures and the progam GOLPE to obtain the partial least squares regression model with the highest prediction ability and forms the basis of a training set suitable for three-dimensional quantitative structure-activity relationship studies.
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Kinetic and crystallographic studies of glucopyranose spirohydantoin and glucopyranosylamine analogs inhibitors of glycogen phosphorylase
TLDR
Four spirohydantoin of glucopyranose and N‐acetyl‐β‐D‐glucopyranosylamine have been identified as the most potent inhibitors of GP that bind at the catalytic site and crystal structures of the analogs in complex with GP were determined.
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The antibody binding site. Labelling of a specific antibody against the photo-precursor of an aryl nitrene.
TLDR
The isolation of specific rabbit antibodies for the haptenic group 4-azido-2-nitrophenyl, is described, indicating that some 13% of the label in the antibody was attached to cysteine-92 and to alanine-93, adjacent to the major hypervariable region in rabbit heavy-chain (residues 95-105).
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Aminosugar derivatives as potential anti-human immunodeficiency virus agents.
TLDR
A method to score in parallel both the degree of antiviral activity and the effect on cell division of aminosugar derivatives suggests that replication is associated with cytolysis, which has important implications in the chemotherapy of AIDS.
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Design of inhibitors of glycogen phosphorylase: a study of alpha- and beta-C-glucosides and 1-thio-beta-D-glucose compounds.
TLDR
It appears that hydration by a water molecule may provide sufficient stabilization to retain the chair conformation and the best inhibitor was N-methyl-beta-glucose-C-carboxamide, which showed a 46-fold improvement in Ki from the parent beta-D-glUCose.
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The isolation by ligand affinity chromatography of a novel form of alpha-L-fucosidase from almond.
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