Unexpected emergence of luciferase-inhibitory activity during structural development study of phenyloxadiazole-based PPAR ligands

Ryuta Shioi, Yosuke Toyota, Tomomi Noguchi-Yachide, Minoru Ishikawa, Takao Yamaguchi, Makoto Makishima, Yuichi Hashimoto, Kenji Ohgane

研究成果: Article査読

2 被引用数 (Scopus)

抄録

Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that regulate transcription of genes involved in lipid, glucose, and cholesterol homeostasis in a ligand-dependent manner. PPARs have long been a target of drug development, and evaluation of PPARs activity frequently involves reporter-gene assay, in which luciferase activity is utilized to visualize transcriptional activation by the receptors. Here, we report our experience of the unexpected emergence of luciferase-inhibitory activity during our search for PPAR antagonists. We believe information about negative experiences like this will help to make medicinal chemists more aware of potential pitfalls in SAR studies with luciferase-based assays.

本文言語English
ページ(範囲)854-864
ページ数11
ジャーナルHeterocycles
97
2
DOI
出版ステータスPublished - 2018
外部発表はい

ASJC Scopus subject areas

  • 分析化学
  • 薬理学
  • 有機化学

フィンガープリント

「Unexpected emergence of luciferase-inhibitory activity during structural development study of phenyloxadiazole-based PPAR ligands」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル