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Nur77 agonists, antagonists and modulators act on Nur77, an orphan receptor of the nuclear receptor family. Its gene is named nuclear receptor subfamily 4 group A member 1 (NR4A1). Nur77 is an immediate early gene product induced by growth factors, stress and T-cell receptor signaling. Besides acting as a transcription factor, Nur77 can move to mitochondria, where it triggers cytochrome c release and apoptosis. A 2008 study identified the fungal metabolite cytosporone B as a Nur77 agonist that binds the ligand-binding domain. The listed compounds include the diindolylmethane analogs DIM-C-pPhOH and DIM-C-pPhCO2Me, which act as NR4A1 antagonists, and the ligand-binding domain antagonist TMPA.
TMPA is a novel small molecule that binds to orphan Nuclear Receptor Nur77 with high affinity (Kd = 1.45 ± 0.35 μM), and interferes with the Nur77-LKB1 interaction.
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. Antineoplastic activity.
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist.
Nur77 Antagonist 1 is a selective antagonist of the Nur77 receptor, with a binding affinity of KDSPR Nur77 = 91 nM. This compound has demonstrated the ability to induce apoptosis in cancer cells, showcasing significant antitumor activity against triple-negative breast cancer (TNBC) cells. It serves as a valuable tool for research in cancer biology and therapeutic development targeting Nur77 pathways.
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