Discovery of new ERRγ agonists regulating dopaminergic neuronal phenotype in SH-SY5Y cells

Bioorganic Chemistry(2022)

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摘要
•We synthesized a series of new ERRγ agonists and found that these compounds were superior or had comparable potencies as DY131 and GSK4716, which are previously reported ERRγ agonists.•5d significantly increased the DAergic neuronal-specific markers, TH and DAT in neuroblastoma SH-SY5Y cells.•5d outstandingly induced DAergic neuronal phenotypes via the ERRγ-mediated up-regulation of CREB-signaling pathway.•Molecular docking study supported the experimental findings for ERRγ agonistic activity of 5d.
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关键词
ERRγ agonist,DAT,TH,CREB,Dopaminergic (DAergic) phenotypes,Neurodegenerative diseases,GSK4716,DY131
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