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

30 April 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

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.

Keywords

Ligand-target engagement
Imaging-based assay
Self-localizing ligand
Protein recruitment
Golgi complex

Supplementary materials

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