β-Arrestin Recruitment Assay for the Identification of Agonists of the Sphingosine 1-Phosphate Receptor EDG1

β-Arrestin recruitment assays provide a generic assay platform for drug discovery on G-protein-coupled receptors (GPCRs). The PathHunter™ assay technology developed by DiscoveRx (Fremont, CA) uses enzyme fragment complementation of β-galactosidase to measure receptor-β-arrestin proximity by chemilum...

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Veröffentlicht in:	Journal of biomolecular screening 2008-12, Vol.13 (10), p.986-998
Hauptverfasser:	Van Der Lee, Miranda M.C., Bras, Maaike, Van Koppen, Chris J., Zaman, Guido J.R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arrestins - metabolism beta-Alanine - analogs & derivatives beta-Alanine - pharmacology beta-Arrestins Biological Assay - methods Cell Differentiation - drug effects CHO Cells Cricetinae Cricetulus Dose-Response Relationship, Drug EDG1 Endothelial Cells - cytology Endothelial Cells - drug effects enzyme fragment complementation Extracellular Signal-Regulated MAP Kinases - metabolism G-protein-coupled receptor GTP-Binding Proteins - metabolism Humans Oxadiazoles - pharmacology Phosphorylation - drug effects Protein Binding - drug effects Receptors, Interleukin-8B - metabolism Receptors, Lysosphingolipid - agonists S1P1 Signal Transduction - drug effects Small Molecule Libraries - analysis Small Molecule Libraries - pharmacology Thiophenes - pharmacology Time Factors β-arrestin β-galactosidase
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