Background
4A7C-301-Nurr1 agonist is an agonist of nuclear receptor-related 1 (Nurr1).1 It binds to the Nurr1 ligand-binding domain (LBD; IC50 = 48.22 nM) and increases transcriptional activity of Nurr1-LBD and full-length Nurr1 in reporter assays using SK-N-BE(2)C human neuroblastoma cells (EC50s = 6.53 and 50-70 μM, respectively). 4A7C-301-Nurr1 agonist (5 mg/kg per day) decreases dopaminergic cell death in the striatum and substantia nigra pars compacta, as well as reduces motor and olfactory deficits, without inducing dyskinesia-like behaviors in mouse models of Parkinson’s disease induced by the neurotoxin MPTP or by overexpression of α-synuclein.
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