An orally bioavailable activator of Nurr1
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C-DIM12 is a synthetic Nurr1 activaor induces Nurr1 and DA gene expression in cell lines and primary neurons.Target: Nurr1in vitro: C-DIM12 as a modulator of Nurr1 activity that results in inhibition of NF-κB-dependent gene expression in glial cells by stabilizing nuclear corepressor proteins, which reduces binding of p65 to inflammatory gene promoters. C-DIM12 Decreases Inflammatory Gene Expression in BV-2 Microglia. C-DIM12 Decreases Expression of NF-κB-Enhanced GFP Expression in Human Embryonic Kidney 293 Reporter Cells.[1] C-DIM12 increases protein levels of exogenously expressed human Nurr1 in transfected neurons.C-DIM12 protects neurons from 6-hydroxydopamine toxicity. [2]
参考文献:
[1]. De Miranda BR, et al. The Nurr1 Activator 1,1-Bis(3'-Indolyl)-1-(p-Chlorophenyl)Methane Blocks Inflammatory Gene Expression in BV-2 Microglial Cells by Inhibiting Nuclear Factor κB. Mol Pharmacol. 2015 Jun;87(6):1021-34. doi: 10.1124/mol.114.095398. Epub
[2]. Hammond SL, et al. A novel synthetic activator of Nurr1 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro. Neurosci Lett. 2015 Oct 21;607:83-9.
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