ArticleActa pharmacologica Sinica2018
Development of a high-throughput fluorescence polarization assay for the discovery of EZH2-EED interaction inhibitors.
Article in Acta pharmacologica Sinica, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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14 citing papers in PubMed, 34 citations in OpenAlex.
- Specificity and exon target space of splicing modifying compounds.Nature communications · 2026Article
- Reduced Maintenance DNA Methylation Thresholds Enable Sensitive Reporter Assays for UHRF1 and DNMT1 Inhibition.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Modulating the Kinetics of a Fluorescence Anisotropy Immunoassay Using Tracer Point Mutations to Measure Human C-Peptide Secretion On-Chip.ACS omega · 2025Article
- Targeting EED as a key PRC2 complex mediator toward novel epigenetic therapeutics.Drug discovery today · 2024Review
- Development of Peptide Displacement Assays to Screen for Antagonists of DDB1 Interactions.Biochemistry · 2024Article
- Identifying ligands for the PHD1 finger of KDM5A through high-throughput screening.RSC chemical biology · 2024Article
- Detection speed optimization of the OI-RD microscope for ultra-high throughput screening.Biomedical optics express · 2023Article
- A Fluorescence-Polarization-Based Lipopolysaccharide-Caspase-4 Interaction Assay for the Development of Inhibitors.Molecules (Basel, Switzerland) · 2022Article
- An overview of the development of EED inhibitors to disable the PRC2 function.RSC medicinal chemistry · 2022Review
- Review
- Identification of novel EED-EZH2 PPI inhibitors using an in silico fragment mapping method.Journal of computer-aided molecular design · 2021Article
- EZH2: a novel target for cancer treatment.Journal of hematology & oncology · 2020Review
- Fluorescence polarization assay for the identification and evaluation of inhibitors at YAP-TEAD protein-protein interface 3.Analytical biochemistry · 2019Article
- Identification of small molecule inhibitors targeting the SMARCA2 bromodomain from a high-throughput screening assay.Acta pharmacologica Sinica · 2018Article
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Aberrant activity of enhancer of zeste homolog 2 (EZH2) is associated with a wide range of human cancers. The interaction of EZH2 with embryonic ectoderm development (EED) is required for EZH2's catalytic activity. Inhibition of the EZH2-EED complex thus represents a novel strategy for interfering with the oncogenic potentials of EZH2 by targeting both its catalytic and non-catalytic functions. To date, there have been no reported high-throughput screening (HTS) assays for inhibitors acting at the EZH2-EED interface. In this study, we developed a fluorescence polarization (FP)-based HTS system for the discovery of EZH2-EED interaction inhibitors. The tracer peptide sequences, positions of fluorescein labeling, and a variety of physicochemical conditions were optimized. The high Z' factors (>0.9) at a variety of DMSO concentrations suggested that this system is robust and suitable for HTS. The minimal sequence requirement for the EZH2-EED interaction was determined by using this system. A pilot screening of an in-house compound library containing 1600 FDA-approved drugs identified four compounds (apomorphine hydrochloride, oxyphenbutazone, nifedipine and ergonovine maleate) as potential EZH2-EED interaction inhibitors.
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