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Ligand design for somatostatin receptor isoforms 4 and 5
(Elsevier, 2018-11-17)
The somatostatin receptor (SSTR) isoforms, SSTR-4 and SSTR-5 are targets in numerous disorders and diseases. Although there has been some success in achieving selective isoform inhibition, structure-based drug design and ...
Anomer preferences for glucuronic and galacturonic acid and derivatives and influence of electron-withdrawing substituents
(American Chemical Society, 2018-07-04)
Equilibrium anomeric ratios are reported for pyranoses (hemiacetals) of glucuronic and galacturonic acid and their derivatives. These are compared to related gluco- and galactopyranoses and to deoxyfluorogluco- and ...
N-Alkyl-1,5-dideoxy-1,5-imino-l-fucitols as fucosidase inhibitors: Synthesis, molecular modelling and activity against cancer cell lines
(Elsevier, 2018-12-04)
1,5-Dideoxy-1,5-imino-l-fucitol (1-deoxyfuconojirimycin, DFJ) is an iminosugar that inhibits fucosidases. Herein, N-alkyl DFJs have been synthesised and tested against the ¿-fucosidases of T. maritima (bacterial origin) ...
Influence of protein (human galectin-3) design on aspects of lectin activity
(Springer, 2020-04-25)
The concept of biomedical significance of the functional pairing between tissue lectins and their glycoconjugate counterreceptors has reached the mainstream of research on the flow of biological information. A major challenge ...
Probing sulfatide-tissue lectin recognition with functionalized glycodendrimersomes
(Cell Press, 2021-01-22)
The small 3-O-sulfated galactose head group of sulfatides, an abundant glycosphingolipid class, poses the (sphinx-like) riddle on involvement of glycan bridging by tissue lectins (sugar code). First, synthesis of head group ...
Microcavity array supported lipid bilayer models of ganglioside – influenza hemagglutinin1 binding
(Royal Society of Chemistry, 2020-08-07)
The binding of influenza receptor (HA(1)) to membranes containing different glycosphingolipid receptors was investigated at Microcavity Supported Lipid Bilayers (MSLBs). We observed that HA(1)preferentially binds to GD1a ...
Development of Mcl-1 inhibitors for cancer therapy
(Elsevier, 2020-11-24)
The myeloid leukemia cell differentiation protein (Mcl-1) is an anti-apoptotic protein of the B-cell lymphoma 2 (Bcl-2) family, which regulates cellular apoptosis. Mcl-1 expression plays a key role in survival of cancer ...
Lewis acid promoted anomerisation of alkyl O- and S-xylo-, arabino- and fucopyranosides
(Elsevier, 2018-11-24)
Pentopyranoside and 6-deoxyhexopyranosides, such as those from d-xylose, l-arabinose and l-fucose are components of natural products, oligosaccharides or polysaccharides. Lewis acid promoted anomerisation of some of their ...
Engineering a therapeutic lectin by uncoupling mitogenicity from antiviral activity
(Elsevier, 2015-10-22)
A key effector route of the Sugar Code involves lectins that exert crucial regulatory controls by targeting distinct cellular glycans. We demonstrate that a¿¿single amino-acid substitution in a banana lectin, replacing ...
Building blocks from monosaccharides for synthesis of scaffolds, including macrocycles. Application of allylic azide rearrangement, azide-alkyne cycloaddition and ring closing metathesis
(Elsevier, 2020-09-18)
Synthesis of compounds with characteristics of natural products are required to increase the diversity and biological relevance of compounds for screening. These include new frameworks/scaffolds, with multiple stereogenic ...