Bochkis Lab

University of Pittsburgh at Pittsburgh

PATHOLOGY

Pittsburgh · United States

NIH-funded
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NIH R01 · 2024

Role of Foxa2 in ligand-dependent activation of nuclear receptors

Project Summary/Abstract Activation of nuclear receptors, a family of ligand-dependent transcription factors, is used extensively in pharmacology to develop drug targets for diverse medical conditions, including metabolic disease and cancer. While synthetic agonists and antagonists of nuclear receptors ameliorate symptoms of many diseases, clinical use of these compounds leads to frequent side effects that range in their severity. Type II receptors, such as FXR, LXR, and PPAR, which function in fatty acid, bile acid, cholesterol, and glucose metabolism, are permanently positioned in the nucleus regardless of the ligand status. The accepted paradigm regarding ligand activation of type II…

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