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Using High Content Imaging to Quantify Target Engagement in Adherent Cells
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Quantifying Target Occupancy of Small Molecules Within Living Cells.

M B Robers1, R Friedman-Ohana1, K V M Huber2,3

  • 1Promega Corporation, Madison, Wisconsin 53711, USA; email: matt.robers@promega.com, rachel.ohana@promega.com, jim.vasta@promega.com.

Annual Review of Biochemistry
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Summary
This summary is machine-generated.

Understanding drug-target interactions in living cells is crucial for developing effective therapeutics. New methods allow precise measurement of target engagement, improving drug discovery and safety profiles.

Keywords:
NanoBRETSARchemical proteomicsenergy transferstructure–activity relationshiptarget engagementtarget occupancy

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Biochemistry

Background:

  • Binding affinity and kinetics are key for structure-activity relationships (SARs) in drug development.
  • Improved target engagement enhances drug efficacy and therapeutic window.
  • Cellular assays are vital for interpreting drug activity and SARs.

Purpose of the Study:

  • To review technological advancements for quantitative target occupancy assessment in living cells.
  • To highlight generalizable methodologies for precise drug binding analysis in cellular environments.
  • To bridge the gap between cellular phenotype and molecular binding properties.

Main Methods:

  • Survey of recent technological advancements in drug binding assays.
  • Emphasis on methodologies applicable to cultured cells.
  • Focus on achieving analytical precision comparable to biochemical methods.

Main Results:

  • Several key technologies now enable quantitative target occupancy measurement in cells.
  • These methods offer improved interpretation of cellular SARs.
  • Advancements provide biochemical-level precision within a cellular context.

Conclusions:

  • Quantitative assessment of drug binding in living cells is integral to modern medicinal chemistry.
  • New methodologies enhance the understanding of drug-target interactions within cells.
  • These advancements facilitate more accurate drug efficacy and safety predictions.