Label-free integrative pharmacology on-target of drugs at the β(2)-adrenergic receptor

• Published in: Scientific reports Vol. 1; p. 33
• Main Authors: Ferrie, Ann M, Sun, Haiyan, Fang, Ye
• Format: Journal Article
• Language: English
• Published: England 2011
• Subjects: Adrenergic beta-2 Receptor Antagonists - pharmacology; Biological Assay - instrumentation; Biosensing Techniques - instrumentation; Cell Separation - instrumentation; Drug Evaluation, Preclinical - instrumentation; Equipment Design; Equipment Failure Analysis; Flow Cytometry - instrumentation; Microfluidic Analytical Techniques - instrumentation; Pharmaceutical Preparations - administration & dosage; Protein Interaction Mapping - instrumentation; Receptors, Adrenergic, beta-2 - drug effects; Staining and Labeling; Systems Integration
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/srep00033

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.