HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter.


Hepatocyte nuclear factor (HNF)4α is a central regulator of gene expression in cell types that play a critical role in metabolic homeostasis, including hepatocytes, enterocytes, and pancreatic β cells. Although fatty acids were found to occupy the HNF4α ligand-binding pocket and were proposed to act as ligands, there is controversy about both the nature of… (More)
DOI: 10.1016/j.chembiol.2012.05.014


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