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

Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

60 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)5080-5093
Number of pages14
JournalBioorganic and Medicinal Chemistry
Volume13
Issue number17
DOIs
Publication statusPublished - Sep 1 2005
Externally publishedYes

Fingerprint

Androgen Receptor Antagonists
Retinoid X Receptors
Retinoic Acid Receptors
Calcitriol Receptors
Peroxisome Proliferator-Activated Receptors
Cytoplasmic and Nuclear Receptors
Binding Sites
Ligands

ASJC Scopus subject areas

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

Cite this

Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis. / Hashimoto, Yuichi; Miyachi, Hiroyuki.

In: Bioorganic and Medicinal Chemistry, Vol. 13, No. 17, 01.09.2005, p. 5080-5093.

Research output: Contribution to journalArticle

Hashimoto, Yuichi ; Miyachi, Hiroyuki. / Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis. In: Bioorganic and Medicinal Chemistry. 2005 ; Vol. 13, No. 17. pp. 5080-5093.
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