Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis

Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

60 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)5080-5093
Number of pages14
JournalBioorganic and Medicinal Chemistry
Issue number17
Publication statusPublished - Sep 1 2005


ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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