Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verification.
|Abstract||The identification of biologically active compounds from high-throughput screening (HTS) can involve considerable postscreening analysis to verify the nature of the sample activity. In this study we evaluated the performance of micro-parallel liquid chromatography (microPLC) as a separation-based enzyme assay platform for follow-up of compound activities found in quantitative HTS of two different targets, a hydrolase and an oxidoreductase. In an ... [truncated at 450 characters in length]|
|Author||Simeonov, Anton; Yasgar, Adam; Klumpp, Carleen; et al|
|Subject||Chromatography, Gas Chromatography, High Pressure Liquid Chromatography, Liquid Dose-Response Relationship, Drug Drug Evaluation, Preclinical Enzyme Activation False Positive Reactions Fluorometry Glucosylceramidase Hydroxymethylglutaryl CoA Reductases Indicators and Reagents Spectrometry, Fluorescence Spectrophotometry, Ultraviolet methods instrumentation methods drug effects analysis metabolism analysis metabolism|
X-ray crystallography of agonist/antagonist-bound receptors.
|Abstract||Crystallographic analysis of the ligand-binding domains of nuclear hormone receptors (NR) has provided a unique insight into the molecular events that underlie the ligand-mediated control of their transcriptional activity. The technique relies on preparing milligram quantities of protein, growing three-dimensional crystals of the desired protein-ligand complex, collecting X-ray diffraction data, and subsequently interpreting the derived electron ... [truncated at 450 characters in length]|
|Author||Pike, Ashley C W;|
|Subject||Crystallization Crystallography, X-Ray Estrogen Receptor alpha Ligands Protein Conformation Receptors, Cytoplasmic and Nuclear instrumentation methods instrumentation methods chemistry metabolism chemistry metabolism|
High-performance liquid chromatography separation and intact mass analysis of detergent-solubilized integral membrane proteins.
|Abstract||We have developed a method for intact mass analysis of detergent-solubilized and purified integral membrane proteins using liquid chromatography-mass spectrometry (LC-MS) with methanol as the organic mobile phase. Membrane proteins and detergents are separated chromatographically during the isocratic stage of the gradient profile from a 150-mm C3 reversed-phase column. The mass accuracy is comparable to standard methods employed for soluble prote ... [truncated at 450 characters in length]|
|Author||Berridge, Georgina; Chalk, Rod; D'Avanzo, Nazzareno; et al|
|Subject||Chromatography Chromatography, High Pressure Liquid Chromatography, Liquid Detergents Mass Spectrometry Membrane Proteins Methanol Spectrometry, Mass, Electrospray Ionization instrumentation methods methods methods chemistry methods chemistry chemistry methods|