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Golgi Recruitment Assay for Visualizing Small-Molecule Ligand–target Engagement in Cells

submitted on 30.04.2020, 05:18 and posted on 30.04.2020, 12:08 by Sachio Suzuki, Masahiro Ikuta, Tatsuyuki Yoshii, Akinobu Nakamura, Keiko Kuwata, Shinya Tsukiji
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.


Email Address of Submitting Author


Nagoya Institute of Technology



ORCID For Submitting Author


Declaration of Conflict of Interest

S.S., M.I., T.Y., A.N., and S.T. are co-inventors on a patent application related to this work. K.K. declares no competing interests.