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Live-Cell Intra-Cellular Quantification of Target Engagement and Compound Residence Time Using a Novel BRET Assay

This Webinar covers:

  • Biochemical vs. cellular analysis of target engagement
  • Use of BRET to directly measure target engagement in live cells
  • Data with specific target proteins (HDACs and kinases) interacting with known inhibitors

Summary

Understanding how a small molecule compound interacts with its target protein is essential for developing successful drugs. Many potential drug candidates have entered clinical trials only to fail due to a poor understanding of how the drug interacts with its target in vivo. In vitro measurements of ligand affinity and duration of drug-target interactions (i.e., residence time) often do not translate in vivo. To bridge this gap, a system that relies on Bioluminescence Resonance Energy Transfer (BRET) to directly measure target engagement inside cells has been developed.

 


Speaker

matt-robers-125x125

Matt Robers
Sr Research Scientist, Group Leader
Promega Corporation

Matthew Robers is a Senior Research Scientist and Group Leader at Promega Corporation. Prior to joining Promega, Matt was focused on pathway analysis in the cell-based assay group at Life Technologies. Matt has authored numerous peer-reviewed publications and published patents on the application of novel fluorescent and bioluminescent chemistries to measure intracellular protein dynamics. The focus of Matt’s team at Promega is to apply new technologies to assess target engagement. Matt’s team has recently developed a biophysical technique for quantifying compound affinity and residence time at selected intracellular targets within intact cells.

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