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7 March 2021 Water-soluble and cell-permeant zwitterionic rhodamine dyes enable quantitative imaging of drug target engagement
Antonio R. Montaño, Lei G. Wang, Allison Solanki, Nathan McMahon, Marcus Kwon, Kenneth M. Tichauer, Kimberley S. Samkoe, Summer L. Gibbs
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Proceedings Volume 11624, Visualizing and Quantifying Drug Distribution in Tissue V; 116240H (2021) https://doi.org/10.1117/12.2582638
Event: SPIE BiOS, 2021, Online Only
Abstract
Intracellular paired-agent imaging (iPAI) utilizes fluorescent-labeled small molecule therapeutics to measure drug target engagement. Our new water-soluble, cell-permeant fluorophores termed Sulfo-Rh and Sulfo-SiRh show substantially improved optical stability against solvent polarity changes over tetramethylrhodamine (TMR) and silicon-substituted TMR, respectively, while retaining the desirable photophysical properties of the base compounds, including brightness, to facilitate stable biological imaging. Targeted and untargeted versions of an EGFR tyrosine kinase inhibitor labeled with these fluorophores, demonstrated similarity to the parent drug in competitive binding and cytotoxicity assays. Utilizing iPAI to visualize drug target engagement enables quantitative small molecule imaging in living systems.
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Antonio R. Montaño, Lei G. Wang, Allison Solanki, Nathan McMahon, Marcus Kwon, Kenneth M. Tichauer, Kimberley S. Samkoe, and Summer L. Gibbs "Water-soluble and cell-permeant zwitterionic rhodamine dyes enable quantitative imaging of drug target engagement", Proc. SPIE 11624, Visualizing and Quantifying Drug Distribution in Tissue V, 116240H (7 March 2021); https://doi.org/10.1117/12.2582638
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KEYWORDS
Rhodamine
Cancer
Imaging systems
Molecules
Resistance
Dynamical systems
Oncology
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