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Related Concept Videos

Protein Dynamics in Living Cells01:19

Protein Dynamics in Living Cells

Different fluorescence-based techniques are used to study the protein dynamics in living cells. These techniques include FRAP, FRET, and PET.
Fluorescent recovery after photobleaching (FRAP) is a fluorescent-protein-based detection technique used to quantify protein movement rates within the cell. This method exposes a small portion of the cell to an intense laser beam. The laser beam causes permanent photobleaching of the fluorophore-tagged proteins in the exposed region. As the bleached...

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A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
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Fluorescence polarization assays in small molecule screening.

Wendy A Lea1, Anton Simeonov

  • 1National Human Genome Research Institute, National Institutes of Health, NIH Chemical Genomics Center, Bethesda, MD 20892-3370, USA.

Expert Opinion on Drug Discovery
|February 14, 2012
PubMed
Summary

Fluorescence polarization (FP) is a versatile tool for analyzing molecular interactions and enzyme activities. Recent advancements show its expanding use in drug discovery and new disease target areas.

Keywords:
Competitive binding assaydrug discoveryenzyme assayfluorescence anisotropyfluorescence polarizationhigh throughput screeningligand displacement

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Area of Science:

  • Biophysics
  • Biochemistry
  • Drug Discovery

Background:

  • Fluorescence polarization (FP) is a homogeneous assay for rapid, quantitative analysis of molecular interactions and enzyme activities.
  • Widely used in clinical diagnostics and therapeutic drug monitoring.
  • Increasingly adopted for high-throughput screening and small molecule drug discovery across diverse targets.

Purpose of the Study:

  • To provide an overview of the theoretical basis of FP.
  • To review recent advancements in FP applications for drug target classes.
  • To discuss assay design, novel applications, and future directions.

Main Methods:

  • Theoretical foundation of FP.
  • Review of recent advancements in FP applications.
  • Discussion of strengths, weaknesses, and practical considerations.

Main Results:

  • Recent advancements in FP applications for GPCRs, enzymes, and protein-protein interactions.
  • Insights into novel applications and future directions for FP in small molecule screening.

Conclusions:

  • FP continues to be vital for high-throughput screening.
  • FP is expanding into new disease and target areas.
  • Increased use of labeled small molecule ligands for receptor-binding studies is a key trend.