title: Label-free integrative pharmacology on-target of drugs at the β(2)-adrenergic receptor.
abstract: We describe a label-free integrative pharmacology on-target (iPOT) method to assess the pharmacology of drugs at the β(2)-adrenergic receptor. This method combines dynamic mass redistribution (DMR) assays using an array of probe molecule-hijacked cells with similarity analysis. The whole cell DMR assays track cell system-based, ligand-directed, and kinetics-dependent biased activities of the drugs, and translates their on-target pharmacology into numerical descriptors which are subject to similarity analysis. We demonstrate that the approach establishes an effective link between the label-free pharmacology and in vivo therapeutic indications of drugs.
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Inc., Corning, NY 14831, USA.
authors.forename: Ann M
authors.initials: AM
authors.lastname: Ferrie
authors.forename: Haiyan
authors.initials: H
authors.lastname: Sun
authors.forename: Ye
authors.initials: Y
authors.lastname: Fang
mesh_terms: D058672:Adrenergic beta-2 Receptor Antagonists / Q000494:pharmacology*; D001681:Biological Assay / Q000295:instrumentation*; D015374:Biosensing Techniques / Q000295:instrumentation*; D002469:Cell Separation / Q000295:instrumentation*; D004353:Drug Evaluation, Preclinical / Q000295:instrumentation; D004867:Equipment Design; D019544:Equipment Failure Analysis; D005434:Flow Cytometry / Q000295:instrumentation; D046210:Microfluidic Analytical Techniques / Q000295:instrumentation*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D025941:Protein Interaction Mapping / Q000295:instrumentation; D018343:Receptors, Adrenergic, beta-2 / Q000187:drug effects*; D013194:Staining and Labeling; D018511:Systems Integration
chemical_list: D058672:Adrenergic beta-2 Receptor Antagonists; D004364:Pharmaceutical Preparations; D018343:Receptors, Adrenergic, beta-2