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Preparation, biochemical characterization and biological properties of radiolabelled N-alkylated deoxynojirimycins.
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. Expand
Inhibition of alpha-L-fucosidase by derivatives of deoxyfuconojirimycin and deoxymannojirimycin.
- B. Winchester, C. Barker, S. Baines, G. Jacob, S. Namgoong, G. Fleet
- Chemistry, Medicine
- The Biochemical journal
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. Expand
Glucose analogue inhibitors of glycogen phosphorylase: the design of potential drugs for diabetes.
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. Expand
POTENT INHIBITION OF GLYCOGEN PHOSPHORYLASE BY A SPIROHYDANTOIN OF GLUCOPYRANOSE : FIRST PYRANOSE ANALOGUES OF HYDANTOCIDIN
Abstract The synthesis of two epimeric spirohydantoins of glucopyranose provides the first examples of pyranose analogues of hydantocidin: molecular modelling correctly predicted that one of the… Expand
Glucose analogue inhibitors of glycogen phosphorylase: from crystallographic analysis to drug prediction using GRID force-field and GOLPE variable selection.
- K. Watson, E. Mitchell, +7 authors S. Zographos
- Biology, Medicine
- Acta crystallographica. Section D, Biological…
- 1 July 1995
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. Expand
Kinetic and crystallographic studies of glucopyranose spirohydantoin and glucopyranosylamine analogs inhibitors of glycogen phosphorylase
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. Expand
The antibody binding site. Labelling of a specific antibody against the photo-precursor of an aryl nitrene.
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). Expand
Aminosugar derivatives as potential anti-human immunodeficiency virus agents.
- A. Karpas, G. Fleet, +5 authors T. Rademacher
- Biology, Medicine
- Proceedings of the National Academy of Sciences…
- 1 December 1988
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. Expand
Design of inhibitors of glycogen phosphorylase: a study of alpha- and beta-C-glucosides and 1-thio-beta-D-glucose compounds.
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. Expand
The isolation by ligand affinity chromatography of a novel form of alpha-L-fucosidase from almond.
- P. Scudder, D. C. Neville, +4 authors G. Jacob
- Chemistry, Medicine
- The Journal of biological chemistry
- 25 September 1990
An alpha-fucosidase has been extracted from almond meal and purified 163,000-fold to apparent homogeneity using a novel affinity ligand, N-(5-carboxy-1-pentyl)-1,5-dideoxy-1,5-imino-L-fucitol,… Expand