2022
DOI: 10.1101/2022.09.19.505646
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Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM

Abstract: Cellular target engagement technologies are reforming drug discovery by enabling quantification of intracellular drug binding; however, concomitant assessment of drug-associated phenotypes has proven challenging. We have developed cellular target engagement by accumulation of mutant (CeTEAM) as a platform that can seamlessly evaluate drug-target interactions and phenotypic responses in a single multiparametric experiment. In the presence of binding ligand, accumulation of an initially unstable target protein a… Show more

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