Evaluation of series of isobenzofuranone dimers as PKCα ligands: Implication for the distance between the two ligand binding sites

Yoshiyasu Baba; Satoshi Mayumi; Go Hirai; Hidekazu Kawasaki; Yosuke Ogoshi; Takeshi Yanagisawa; Yuichi Hashimoto; Mikiko Sodeoka

doi:10.1016/j.bmcl.2004.02.098

Evaluation of series of isobenzofuranone dimers as PKCα ligands: Implication for the distance between the two ligand binding sites

Yoshiyasu Baba, Satoshi Mayumi, Go Hirai, Hidekazu Kawasaki, Yosuke Ogoshi, Takeshi Yanagisawa, Yuichi Hashimoto, Mikiko Sodeoka

Research output: Contribution to journal › Article › peer-review

14 Citations (Scopus)

Abstract

Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl chain dimers having a C₁₀-C₁₂ linker and for the C7 dimers having a C₁₄-C₁₆.

Original language	English
Pages (from-to)	2969-2972
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2004.02.098
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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10.1016/j.bmcl.2004.02.098

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title = "Evaluation of series of isobenzofuranone dimers as PKCα ligands: Implication for the distance between the two ligand binding sites",

abstract = "Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl chain dimers having a C10-C12 linker and for the C7 dimers having a C14-C16.",

author = "Yoshiyasu Baba and Satoshi Mayumi and Go Hirai and Hidekazu Kawasaki and Yosuke Ogoshi and Takeshi Yanagisawa and Yuichi Hashimoto and Mikiko Sodeoka",

note = "Funding Information: This work was supported in part by grants from Uehara Memorial Foundation, and Hoh-ansha Foundation, Kanagawa Academy of Science and Technology Research Grants, a Grant-in-Aid for Creative Scientific Research (No 13NP0401) and a Grant-in-Aid for Scientific Research from the Japan Society for the Promotion of Science, and a Grant-in-Aid for the COE project, Giant Molecules and Complex Systems, from The Ministry of Education, Culture, Sports, Science, and Technology.",

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doi = "10.1016/j.bmcl.2004.02.098",

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T1 - Evaluation of series of isobenzofuranone dimers as PKCα ligands

T2 - Implication for the distance between the two ligand binding sites

AU - Baba, Yoshiyasu

AU - Mayumi, Satoshi

AU - Hirai, Go

AU - Kawasaki, Hidekazu

AU - Ogoshi, Yosuke

AU - Yanagisawa, Takeshi

AU - Hashimoto, Yuichi

AU - Sodeoka, Mikiko

N1 - Funding Information: This work was supported in part by grants from Uehara Memorial Foundation, and Hoh-ansha Foundation, Kanagawa Academy of Science and Technology Research Grants, a Grant-in-Aid for Creative Scientific Research (No 13NP0401) and a Grant-in-Aid for Scientific Research from the Japan Society for the Promotion of Science, and a Grant-in-Aid for the COE project, Giant Molecules and Complex Systems, from The Ministry of Education, Culture, Sports, Science, and Technology.

PY - 2004/6/7

Y1 - 2004/6/7

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AB - Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. To examine the distance between the two ligand binding sites (C1A and C1B) of PKC, we designed and synthesized two series of isobenzofuranone dimers. Peak binding activities were observed for the C3-acyl chain dimers having a C10-C12 linker and for the C7 dimers having a C14-C16.

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Evaluation of series of isobenzofuranone dimers as PKCα ligands: Implication for the distance between the two ligand binding sites

Abstract

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