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

Research output: Contribution to journalArticle

30 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)2963-2967
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number11
DOIs
Publication statusPublished - Jun 7 2004
Externally publishedYes

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All Science Journal Classification (ASJC) codes

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

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