Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists

Jun ichi Kasuga, Seiichi Ishida, Daisuke Yamasaki, Makoto Makishima, Takefumi Doi, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

We designed and synthesized novel PPARδ antagonists based on the crystal structure of the PPARδ full agonist TIPP-204 bound to the PPARδ ligand-binding domain, in combination with our nuclear receptor helix 12 folding modification hypothesis. Representative compound 3a exhibits PPARδ-preferential antagonistic activity.

Original languageEnglish
Pages (from-to)6595-6599
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number23
DOIs
Publication statusPublished - Dec 1 2009

Fingerprint

Peroxisome Proliferator-Activated Receptors
Acids
Cytoplasmic and Nuclear Receptors
Crystal structure
Ligands

Keywords

  • Biphenylcarboxylic acid
  • PPAR
  • PPARδ
  • PPARδ antagonist

ASJC Scopus subject areas

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

Cite this

Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists. / Kasuga, Jun ichi; Ishida, Seiichi; Yamasaki, Daisuke; Makishima, Makoto; Doi, Takefumi; Hashimoto, Yuichi; Miyachi, Hiroyuki.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 23, 01.12.2009, p. 6595-6599.

Research output: Contribution to journalArticle

Kasuga, JI, Ishida, S, Yamasaki, D, Makishima, M, Doi, T, Hashimoto, Y & Miyachi, H 2009, 'Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 23, pp. 6595-6599. https://doi.org/10.1016/j.bmcl.2009.10.021
Kasuga, Jun ichi ; Ishida, Seiichi ; Yamasaki, Daisuke ; Makishima, Makoto ; Doi, Takefumi ; Hashimoto, Yuichi ; Miyachi, Hiroyuki. / Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 23. pp. 6595-6599.
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