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

preprint
submitted on 30.04.2020 and posted on 30.04.2020 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.

History

Email Address of Submitting Author

stsukiji@nitech.ac.jp

Institution

Nagoya Institute of Technology

Country

Japan

ORCID For Submitting Author

0000-0002-1402-5773

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.

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