Pharmacological characterization of a novel negative allosteric modulator of NMDA receptors, UBP792.

N-methyl-d-aspartate (NMDA) receptors (NMDARs) are a subtype of ionotropic glutamate receptor with important roles in CNS function. Since excessive NMDAR activity can lead to neuronal cell death and epilepsy, there is interest in developing NMDAR negative allosteric modulators (NAMs) as neuroprotective agents. In this study, we characterize the inhibitory properties of a novel NMDAR antagonist, UBP792.

Probing sialoglycans on fetal bovine fetuin with azido-sugars using glycosyltransferases.

Sialic acids are negatively charged sugar residues commonly found on the terminal positions of most glycoproteins. They play important roles in the stability and solubility of these proteins. Due to their unique positioning, they also frequently act as receptors for various ligands, and therefore are involved in numerous cell-cell and cell-pathogen interactions.

Glycoprotein labeling with click chemistry (GLCC) and carbohydrate detection.

Molecular labeling and detection techniques are essential to research in life science. Here, a method for glycoprotein labeling/carbohydrate detection through glycan replacement, termed glycoprotein labeling with click chemistry (GLCC), is described. In this method, a glycoprotein is first treated with specific glycosidases to remove certain sugar residues, a procedure that creates acceptor sites for a specific glycosyltransferase.

Development of a comprehensive set of P2 receptor pharmacological research compounds.

Pharmacological manipulation of P2X and P2Y receptors has been critical to the elucidation of the biological roles of these receptors within a multitude of physiological and pathological processes. Initial purinergic signalling research made use of compounds based on pyridoxal phosphate, suramin and nucleotide analogues; recently developed compounds are often derivatives of these early tools. Tocris Bioscience first entered the field of purinergic signalling reagents with the commercial release of the pyridoxal phosphate derivative, iso-PPADS.