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Updated: May 29, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Design, synthesis, and biological evaluation of FXR/ASK1 dual-target modulators
Xi Zhang1, Jingyan Wang1, Ziqiang Zhao1
1School of Pharmacy, Hangzhou Medical College, Hangzhou, 310014, P. R. China.
Abstract:
The dual modulation of FXR and ASK1 is considered a promising therapeutic strategy for metabolic dysfunction-associated fatty liver disease (MAFLD) and its progressive form, metabolic dysfunction-associated steatohepatitis (MASH). GW4064 and GS-4997 are effective regulators for FXR and ASK1, respectively. Through the effective functional group splicing strategy, a new dual-target modulator is designed. Compound Z8, which acts on both targets, was found to more potently reduce intracellular lipid droplet accumulation in OA-treated HepG2 cells than the FXR agonist GW4064 and the ASK1 inhibitor selonsertib (GS-4997).
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