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Updated: Jul 15, 2026

12:38
Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells
Published on: November 6, 2021
[Establishment of a cell-based high-throughput screening model for PPARdelta agonists]
Guo-Ping Lu1, Zhi-Hui Zheng, Bao-Hua Zhao
1College of Life Sciences, Hebei Normal University, Shijiazhuang 050016, China.
Summary
A novel high-throughput screening model for PPARdelta agonists was developed using luciferase reporter assays. This method efficiently identifies potential anti-atherosclerosis and anti-adiposity drug candidates.
Area of Science:
- Molecular Biology
- Drug Discovery
Context:
- Peroxisome proliferator-activated receptor delta (PPARdelta) plays a role in metabolic regulation.
- Identifying PPARdelta agonists is crucial for developing treatments for metabolic disorders.
Purpose:
- To establish and optimize a high-throughput screening (HTS) model for PPARdelta agonists.
- To facilitate the discovery of novel therapeutic agents targeting PPARdelta.
Summary:
- A PPARdelta expression vector and a PPRE-luciferase reporter vector were constructed.
- Co-transfection into cell lines and luciferase assays established a functional HTS model.
- Bezafibrate and linoleic acid demonstrated dose-dependent induction of luciferase, validating the model.
Impact:
- Enables rapid screening of large compound libraries for PPARdelta agonists.
- Potential to accelerate the development of new drugs for atherosclerosis and obesity.
- Provides a valuable tool for metabolic disease research.

