Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM.

doi:10.1038/s41467-024-54415-7

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Article

Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM.

Nature communications - 6 Dec 2024

Valerie Nicholas C K, Sanjiv Kumar, Mortusewicz Oliver, Zhang Si Min, Alam Seher, Pires Maria J, Stigsdotter Hannah, Rasti Azita, Langelier Marie-France, Rehling Daniel, Throup Adam, Purewal-Sidhu Oryn, Desroses Matthieu, Onireti Jacob, Wakchaure Prasad, Almlöf Ingrid, Boström Johan, Bevc Luka, Benzi Giorgia, Stenmark Pål, Pascal John M, Helleday Thomas, Page Brent D G, Altun Mikael

Abstract excerpt

Cellular target engagement technologies enable quantification of intracellular drug binding; however, simultaneous assessment of drug-associated phenotypes has proven challenging. Here, we present cellular target engagement by accumulation of mutant as a platform that can concomitantly evaluate drug-target interactions and phenotypic responses using conditionally stabilized drug biosensors. We observe that...

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PMID: 39643609
DOI: 10.1038/s41467-024-54415-7
PMCID: PMC11624193

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