Date published: 2025-9-18

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NR5A2 Inhibitors

NR5A2 inhibitors are a class of compounds that may reduce the activity of NR5A2 by various mechanisms. They may bind directly to NR5A2 and interfere with its ability to regulate gene transcription, as is the case with molecules like GSK2033, which binds to the ligand-binding domain of NR5A2. Others, like SR1848, function as inverse agonists and could repress NR5A2-mediated transcriptional activity.

Some inhibitors may alter the cellular signaling pathways that affect the expression or post-translational modifications of NR5A2. For example, compounds that inhibit PI3K/AKT signaling, such as LY294002, could lead to downstream effects that decrease NR5A2 activity. Similarly, changes in cholesterol metabolism and transport caused by agents like U18666A could affect the regulatory roles of NR5A2. Moreover, there are compounds that may influence NR5A2 activity indirectly by affecting related pathways or gene expressions, such as tamoxifen and GW9662. These molecules might modulate the expression of genes that overlap with those regulated by NR5A2, leading to altered NR5A2 function. Additionally, broad-spectrum agents like histone deacetylase inhibitors (e.g., valproic acid) could change the expression patterns of genes controlled by NR5A2, potentially leading to repression of NR5A2-regulated genes.

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