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

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 as...

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Published inScientific reports Vol. 1; p. 33
Main Authors Ferrie, Ann M, Sun, Haiyan, Fang, Ye
Format Journal Article
LanguageEnglish
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
Online AccessGet full text
ISSN2045-2322
2045-2322
DOI10.1038/srep00033

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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.
AbstractList 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.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.
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.
Author Sun, Haiyan
Ferrie, Ann M
Fang, Ye
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SubjectTerms 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
Title Label-free integrative pharmacology on-target of drugs at the β(2)-adrenergic receptor
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