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

doi:10.1016/j.bmcl.2004.02.097

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 journal › Article › peer-review

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 language	English
Pages (from-to)	2963-2967
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2004.02.097
Publication status	Published - Jun 7 2004
Externally published	Yes

All Science Journal Classification (ASJC) codes

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

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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 journal › Article › peer-review

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AU - Hashimoto, Yuichi

AU - Sodeoka, Mikiko

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