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A New Era for PPARγ: Covalent Ligands and Therapeutic Applications

Peroxisome proliferator-activated receptor γ (PPARγ) is a prominent ligand-inducible transcription factor involved in adipocyte differentiation, glucose homeostasis, insulin sensitivity, inflammation, and cell proliferation, making it a therapeutic target for diabetes, metabolic syndrome, autoimmune diseases, and cancer. 

Citation:
Smithers L, Vrielink A, Lesterhuis WJ, Piggott MJ. A New Era for PPARγ: Covalent Ligands and Therapeutic Applications. J Med Chem. 2025;68(22):23705-50.

Keywords:
Drug discovery; ligands; ppargamma; agonists; chemistry; metabolism

Abstract:
Peroxisome proliferator-activated receptor γ (PPARγ) is a prominent ligand-inducible transcription factor involved in adipocyte differentiation, glucose homeostasis, insulin sensitivity, inflammation, and cell proliferation, making it a therapeutic target for diabetes, metabolic syndrome, autoimmune diseases, and cancer.