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Issue 57, 2020
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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., 2020,56, 7961-7964
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, 56, 7961 DOI: 10.1039/D0CC02020F

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