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

29 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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Structure-Activity Relationship
Protein Kinase C
Ligands
Derivatives
Signal transduction
Glycerol
Signal Transduction
Enzymes

All Science Journal Classification (ASJC) codes

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

Cite this

Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C. / Baba, Yoshiyasu; Ogoshi, Yosuke; Hirai, Go; Yanagisawa, Takeshi; Nagamatsu, Kumiko; Mayumi, Satoshi; Hashimoto, Yuichi; Sodeoka, Mikiko.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 11, 07.06.2004, p. 2963-2967.

Research output: Contribution to journalArticle

Baba, Yoshiyasu ; Ogoshi, Yosuke ; Hirai, Go ; Yanagisawa, Takeshi ; Nagamatsu, Kumiko ; Mayumi, Satoshi ; Hashimoto, Yuichi ; Sodeoka, Mikiko. / Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C. In: Bioorganic and Medicinal Chemistry Letters. 2004 ; Vol. 14, No. 11. pp. 2963-2967.
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