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Golgi recruitment assay for visualizing small-molecule ligand–target engagement in cells

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Abstract

The development of methods that allow detection of ligand–target engagement in cells is an important challenge in chemical biology and drug discovery. Here, we present a Golgi recruitment (G-REC) assay in which the ligand binding to the target protein can be visualized as Golgi-localized fluorescence signals. We show that the G-REC assay is applicable to the detection of various ligand–target interactions, ligand affinity comparison among distinct protein isoforms, and the monitoring of unmodified drug–target engagement in cells.

Graphical abstract: Golgi recruitment assay for visualizing small-molecule ligand–target engagement in cells

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Supplementary files

Article information


Submitted
18 Mar 2020
Accepted
02 Jun 2020
First published
15 Jun 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

Golgi recruitment assay for visualizing small-molecule ligand–target engagement in cells

S. Suzuki, M. Ikuta, T. Yoshii, A. Nakamura, K. Kuwata and S. Tsukiji, Chem. Commun., 2020, Advance Article , DOI: 10.1039/D0CC02020F

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