Quantitative fluorescence imaging of tyrosine kinase inhibitors in live cells and tissues (Conference Presentation)

Le résumé fourni par la source

Intracellular drug target validation and target engagement quantification have proven to be challenging, and all drugs have some degree of non-specific accumulation due to variable drug affinity, biodistribution, pharmacokinetics, and metabolism. A dynamic ratiometric imaging approach for estimating the concentration of cell surface receptors, termed Paired Agent Imaging, could have a revitalizing effect on quantitative intracellular protein receptor imaging, offering a potential means for quantifying intracellular drug target availability. We have developed a dynamic, fluorescence-based, three-compartment model termed intracellular paired-agent imaging that utilizes fluorophore labeled small molecule therapeutics as imaging agents to measure drug target availability in live cells and tissues.

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