Search Results - "Aristotelous, Tonia"
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Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor
Published in ACS medicinal chemistry letters (10-10-2013)“…G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for about a quarter of all drug targets of approved…”
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Surface plasmon resonance analysis of seven-transmembrane receptors
Published in Methods in enzymology (2015)“…G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for around a third of all drug targets of approved…”
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A mutant O-GlcNAcase enriches Drosophila developmental regulators
Published in Nature chemical biology (01-08-2017)“…An inactive mutant of a bacterial O-GlcNAc hydrolase was used as an affinity reagent to enrich O -GlcNAc-modified proteins from Drosophila embryos and led to…”
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Surveying GPCR solubilisation conditions using surface plasmon resonance
Published in Analytical biochemistry (01-09-2018)“…Biophysical screening techniques, such as surface plasmon resonance, enable detailed kinetic analysis of ligands binding to solubilised G-protein coupled…”
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O-GlcNAc transferase invokes nucleotide sugar pyrophosphate participation in catalysis
Published in Nature chemical biology (01-12-2012)“…OGT modifies numerous proteins with O -GlcNAc, but the mechanism for this reaction has been difficult to define. Ternary crystal structures and activity assays…”
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A biophysical approach for the study of g-protein coupled receptor complexes
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Dissertation -
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Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening
Published in ACS medicinal chemistry letters (08-12-2016)“…The discovery of novel bromodomain inhibitors by fragment screening is complicated by the presence of dimethyl sulfoxide (DMSO), an acetyl-lysine mimetic, that…”
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O‑GlcNAcase Fragment Discovery with Fluorescence Polarimetry
Published in ACS chemical biology (18-05-2018)“…The attachment of the sugar N-acetyl-D-glucosamine (GlcNAc) to specific serine and threonine residues on proteins is referred to as protein O-GlcNAcylation…”
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A Novel Allosteric Inhibitor of the Uridine Diphosphate N‑Acetylglucosamine Pyrophosphorylase from Trypanosoma brucei
Published in ACS chemical biology (20-09-2013)“…Uridine diphosphate N-acetylglucosamine pyrophosphorylase (UAP) catalyzes the final reaction in the biosynthesis of UDP-GlcNAc, an essential metabolite in many…”
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Journal Article