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

doi:10.1016/j.bmcl.2009.10.021

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 journal › Article › peer-review

21 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 language	English
Pages (from-to)	6595-6599
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2009.10.021
Publication status	Published - Dec 1 2009
Externally published	Yes

Keywords

Biphenylcarboxylic acid
PPAR
PPARδ
PPARδ antagonist

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2009.10.021

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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.",

keywords = "Biphenylcarboxylic acid, PPAR, PPARδ, PPARδ antagonist",

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AU - Kasuga, Jun ichi

AU - Ishida, Seiichi

AU - Yamasaki, Daisuke

AU - Makishima, Makoto

AU - Doi, Takefumi

AU - Hashimoto, Yuichi

AU - Miyachi, Hiroyuki

PY - 2009/12/1

Y1 - 2009/12/1

N2 - 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.

AB - 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.

KW - Biphenylcarboxylic acid

KW - PPAR

KW - PPARδ

KW - PPARδ antagonist

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U2 - 10.1016/j.bmcl.2009.10.021

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JF - Bioorganic and Medicinal Chemistry Letters

IS - 23

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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