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  • Title: Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis.
    Author: Hashimoto Y, Miyachi H.
    Journal: Bioorg Med Chem; 2005 Sep 01; 13(17):5080-93. PubMed ID: 16051104.
    Abstract:
    Here we review our studies on the molecular design of nuclear receptor antagonists, including retinoic acid receptor (RAR) antagonists, retinoid X receptor (RXR) antagonists, androgen receptor (AR) antagonists, and vitamin D receptor (VDR) antagonists, based on inhibition of folding of helix 12, which contains a co-activator binding site. Recent progress in structural development studies of peroxisome proliferator-activated receptor (PPAR) ligands is also reviewed.
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