Stockmann, Henning; Todorovic, Viktor; Richardson, Paul L.; Marin, Violeta; Scott, Victoria; Gerstein, Clare; Lake, Marc; Wang, Leyu; Sadhukhan, Ramkrishna; Vasudevan, Anil published the artcile< Cell-Surface Receptor-Ligand Interaction Analysis with Homogeneous Time-Resolved FRET and Metabolic Glycan Engineering: Application to Transmembrane and GPI-Anchored Receptors>, Safety of 1,3-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, the main research area is cell surface receptor ligand interaction FRET glycan engineering; transmembrane GPI anchored receptor FRET glycan engineering.
Ligand-binding assays are the linchpin of drug discovery and medicinal chem. Cell-surface receptors and their ligands have traditionally been characterized by radioligand-binding assays, which have low temporal and spatial resolution and entail safety risks. Here, the authors report a powerful alternative (GlycoFRET), where terbium-labeled fluorescent reporters are irreversibly attached to receptors by metabolic glycan engineering. For the first time, the authors show time-resolved fluorescence resonance energy transfer between receptor glycans and fluorescently labeled ligands. The authors describe GlycoFRET for a GPI-anchored receptor, a G-protein-coupled receptor, and a heterodimeric cytokine receptor in living cells with excellent sensitivity and high signal-to-background ratios. In contrast to previously described methods, GlycoFRET does not require genetic engineering or antibodies to label receptors. Given that all cell-surface receptors are glycosylated, the authors expect that GlycoFRET can be generalized with applications in chem. biol. and biotechnol., such as target engagement, receptor pharmacol., and high-throughput screening.
Journal of the American Chemical Society published new progress about Cell membrane. 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Safety of 1,3-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics