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Updated: Jun 16, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
Published on: December 11, 2016
[PPARgamma targeted genome-based drug discovery; present and future direction]
1Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University.
Peroxisome proliferator-activated receptors (PPARs) regulate crucial biological processes. Medicinal chemistry efforts focus on designing selective PPAR ligands for therapeutic applications in metabolic and inflammatory diseases.
Area of Science:
- Biochemistry and Molecular Biology
- Medicinal Chemistry
- Pharmacology
Context:
- Peroxisome proliferator-activated receptor gamma (PPARgamma) initially identified for adipocyte differentiation.
- PPARs are now recognized as pleiotropic regulators involved in lipid, glucose homeostasis, inflammation, and cell proliferation.
- Glitazones, a class of antidiabetic drugs, target PPARgamma.
Purpose:
- To summarize recent medicinal chemistry advancements in the design and synthesis of PPAR-related agents.
- To highlight the development of novel PPAR ligands with subtype selectivity.
- To explore the therapeutic potential of PPAR ligands for various diseases.
Summary:
- Recent genome-wide analyses reveal PPARs as key regulators of diverse biological responses beyond lipid metabolism.
- Medicinal chemistry is actively pursuing the development of selective PPAR ligands.
- These novel ligands serve as research tools and potential therapeutic candidates for PPARs-mediated conditions.
Impact:
- Development of novel therapeutic agents targeting PPARs for metabolic diseases, inflammation, and cancer.
- Enhanced understanding of PPARs' complex roles in human physiology and disease.
- Advancement of chemical biology tools for investigating PPAR function.
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