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Quantitative, Real-Time Measurements of Intracellular Target Engagement Using Energy Transfer

Authors :
Matthew B, Robers
James D, Vasta
Cesear R, Corona
Rachel Friedman, Ohana
Robin, Hurst
Manisha A, Jhala
Kenneth M, Comess
Keith V, Wood
Source :
Methods in molecular biology (Clifton, N.J.). 1888
Publication Year :
2018

Abstract

Intracellular target affinity and residence time are fundamental aspects of pharmacological mechanism (Lu and Tonge, Curr Opin Chem Biol 14:467-474, 2010). Although various robust biochemical approaches exist to measure these binding characteristics, analysis of compound binding with isolated targets may not accurately reflect engagement in the milieu of living cells. To realize the influence of cellular context, methods are needed that are capable of quantifying affinity and residence time in the presence of the intracellular factors that may impact target engagement. Bioluminescence resonance energy transfer (BRET) offers a solution for intracellular target engagement when quantitative metrics or kinetic analyses are required.

Details

ISSN :
19406029
Volume :
1888
Database :
OpenAIRE
Journal :
Methods in molecular biology (Clifton, N.J.)
Accession number :
edsair.pmid..........9325d2a9b4856f15ce689352bb07bd94