Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C

Yoshiyasu Baba, Yosuke Ogoshi, Go Hirai, Takeshi Yanagisawa, Kumiko Nagamatsu, Satoshi Mayumi, Yuichi Hashimoto, Mikiko Sodeoka

研究成果: Contribution to journalArticle査読

31 被引用数 (Scopus)

抄録

Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. We have designed novel PKC ligands having an isobenzofuranone template, based on the proposed interaction of DAG (1,2-diacyl-sn-glycerol) with the PKCδ C1B ligand-binding domain. Several isobenzofuranone derivatives were synthesized and their PKCα binding activities were evaluated. The pivaloyl derivative 1f was found to be a strong PKCα ligand, and the structure-activity relationship is well explained by our proposed binding model.

本文言語英語
ページ(範囲)2963-2967
ページ数5
ジャーナルBioorganic and Medicinal Chemistry Letters
14
11
DOI
出版ステータス出版済み - 6 7 2004
外部発表はい

All Science Journal Classification (ASJC) codes

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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