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Updated: Sep 29, 2025
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High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
Published on: March 3, 2015
9.6K
High throughput screening for compounds to the orphan nuclear receptor NR2F6
Emery Smith1, Sean Campbell2, Adrianna N Wilson3
1Department of Molecular Medicine, The Scripps Research Institute, Scripps Florida, 130 Scripps Way, Jupiter, FL, 33458, USA.
SLAS Discovery : Advancing Life Sciences R & D
|March 25, 2022
Summary
Researchers identified small molecules targeting NR2F6, a novel immune checkpoint in cancer. This discovery holds potential for developing new immuno-oncology therapeutics to combat cancer by modulating NR2F6 activity.
Area of Science:
- Oncology
- Immunology
- Molecular Biology
Background:
- Nuclear Receptor NR2F6 is an orphan receptor implicated in cancer.
- NR2F6 functions as an immune checkpoint in effector T cells.
- NR2F6 is upregulated in various cancers, suggesting therapeutic potential.
Purpose of the Study:
- To identify small molecule regulators of NR2F6 transcriptional activity.
- To explore NR2F6 as a target for immuno-oncology drug development.
Main Methods:
- Developed a high-throughput cell-based assay to measure NR2F6 activity.
- Screened approximately 666,000 compounds.
- Utilized counterscreening assays to confirm hits.
Main Results:
- Identified 5,008 initial hit compounds from the screen.
- Confirmed 128 compounds with IC50 values ≤ 5μM.
- Reported the first small molecules identified for the orphan nuclear receptor NR2F6.
Conclusions:
- Small molecule modulators of NR2F6 were successfully identified.
- These compounds represent potential therapeutic agents for cancer treatment.
- NR2F6 modulation offers a promising strategy in immuno-oncology.
