A high-throughput screen for inhibitors of the prolyl isomerase, Pin1, identifies a seaweed polyphenol that reduces adipose cell differentiation
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- Tadashi Mori
- Molecular Enzymology, Department of Molecular Cell Science, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
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- Masafumi Hidaka
- Molecular Enzymology, Department of Molecular Cell Science, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
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- Hiroko Ikuji
- Molecular Enzymology, Department of Molecular Cell Science, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
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- Ibuki Yoshizawa
- Molecular Enzymology, Department of Molecular Cell Science, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
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- Haruhiko Toyohara
- Graduate School of Agriculture, Kyoto University, Kyoto, Japan
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- Toru Okuda
- Tamagawa University, Research Center, Tokyo, Japan
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- Chiyoko Uchida
- Department of Human Development and Culture, Fukushima University, Fukushima, Japan
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- Tomoichiro Asano
- Department of Medical Science, Graduate School of Medicine, University of Hiroshima, Hiroshima, Japan
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- Mari Yotsu-Yamashita
- Bioorganic Chemistry of Natural Products, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
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- Takafumi Uchida
- Molecular Enzymology, Department of Molecular Cell Science, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
説明
<jats:title>Abstract</jats:title> <jats:p>The peptidyl prolyl cis/trans isomerase Pin1 enhances the uptake of triglycerides and the differentiation of fibroblasts into adipose cells in response to insulin stimulation. Pin1 downregulation could be a potential approach to prevent and treat obesity-related disorders. In order to identify an inhibitor of Pin1 that exhibited minimal cytotoxicity, we established a high-throughput screen for Pin1 inhibitors and used this method to identify an inhibitor from 1,056 crude fractions of two natural product libraries. The candidate, a phlorotannin called 974-B, was isolated from the seaweed, Ecklonia kurome. 974-B inhibited the differentiation of mouse embryonic fibroblasts and 3T3-L1 cells into adipose cells without inducing cytotoxicity. We discovered the Pin1 inhibitor, 974-B, from the seaweed, E. kurome, and showed that it blocks the differentiation of fibroblasts into adipose cells, suggesting that 974-B could be a lead drug candidate for obesity-related disorders.</jats:p>
収録刊行物
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- Bioscience, Biotechnology, and Biochemistry
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Bioscience, Biotechnology, and Biochemistry 78 (5), 832-838, 2014-05-04
Informa UK Limited
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詳細情報 詳細情報について
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- CRID
- 1360848659102186880
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- ISSN
- 13476947
- 09168451
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