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  1. 学部学科区分一覧
  2. 医学部・医学系研究科・医学部附属病院
  1. 資料タイプ一覧
  2. 学術雑誌論文
  1. 鳥取大学の刊行物
  2. Yonago Acta Medica
  3. 63
  4. 1

Identification of a Novel Deactivating Small-Molecule Compound for Fibrogenic Hepatic Stellate Cells

https://repository.lib.tottori-u.ac.jp/records/4721
https://repository.lib.tottori-u.ac.jp/records/4721
67e4b62c-03bb-4ee4-9670-2a57640f9a3f
名前 / ファイル ライセンス アクション
yam63(1)_79.pdf yam63(1)_79.pdf (2.0 MB)
Item type 学術雑誌論文 / Journal Article(1)
公開日 2020-02-28
タイトル
タイトル Identification of a Novel Deactivating Small-Molecule Compound for Fibrogenic Hepatic Stellate Cells
言語 en
言語
言語 eng
キーワード
主題Scheme Other
主題 deactivation
キーワード
主題Scheme Other
主題 hepatic stellate cells
キーワード
主題Scheme Other
主題 liver fibrosis
キーワード
主題Scheme Other
主題 small-molecule compound
キーワード
言語 en
主題Scheme Other
主題 deactivation
キーワード
言語 en
主題Scheme Other
主題 hepatic stellate cells
キーワード
言語 en
主題Scheme Other
主題 liver fibrosis
キーワード
言語 en
主題Scheme Other
主題 small-molecule compound
資源タイプ
資源タイプ journal article
著者 Sakaguchi, Takuki

× Sakaguchi, Takuki

en Sakaguchi, Takuki

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Kono, Yohei

× Kono, Yohei

en Kono, Yohei

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Itaba, Noriko

× Itaba, Noriko

en Itaba, Noriko

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Morimoto, Minoru

× Morimoto, Minoru

en Morimoto, Minoru

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Isomoto, Hajime

× Isomoto, Hajime

en Isomoto, Hajime

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Shiota, Goshi

× Shiota, Goshi

en Shiota, Goshi

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著者所属(英)
言語 en
値 Department of Genetic Medicine and Regenerative Therapeutics, Graduate School of Medical Sciences, Tottori University / Division of Medicine and Clinical Science, Department of Multidisciplinary Internal Medicine, School of Medicine, Tottori University Faculty of Medicine
著者所属(英)
言語 en
値 Department of Genetic Medicine and Regenerative Therapeutics, Graduate School of Medical Sciences, Tottori University
著者所属(英)
言語 en
値 Department of Genetic Medicine and Regenerative Therapeutics, Graduate School of Medical Sciences, Tottori University
著者所属(英)
言語 en
値 Research Initiative Center, Tottori University
著者所属(英)
言語 en
値 Division of Medicine and Clinical Science, Department of Multidisciplinary Internal Medicine, School of Medicine, Tottori University Faculty of Medicine
著者所属(英)
言語 en
値 Department of Genetic Medicine and Regenerative Therapeutics, Graduate School of Medical Sciences, Tottori University
抄録
内容記述タイプ Other
内容記述 Background: Liver fibrosis progresses to decompensated liver cirrhosis, for which medical needs remain unmet. We recently developed IC-2, a small-molecule compound that suppresses Wnt/β-catenin signaling, and found that IC-2 also suppresses liver fibrosis. In this study, we performed three-step screening of newly synthesized IC-2 derivatives to identify other small-molecule compounds that suppress liver fibrosis. Methods: The screening system consisted of three steps: a cell viability assay, a transcription factor 4 (TCF4) reporter assay, and induction of α-smooth muscle actin (α-SMA) and collagen 1α1 (Col1A1) expression in response to each compound. Screening using human LX-2 hepatic stellate cells (HSCs) was performed to target HSCs, which are the driver cells of liver fibrosis. Results: In the first step, since 9b and 9b-CONH2 at 100 μM did not have any effects on cell viability, they were omitted in the next screening. Additionally, the conditions that led to > 40% inhibition of the controls were also excluded in subsequent screening. The second step was performed under 31 conditions for 19 small-molecule compounds. Sixteen small-molecule compounds caused significant reduction of TCF4 activity relative to that of 0.1% DMSO. Of the 16 compounds, the 10 showing the greatest suppression of TCF4 activity were selected for the third step. Expressions of mRNA for α-SMA and Col1A1 were significantly reduced by seven and three small-molecule compounds, respectively. The greatest reductions in the α-SMA and Col1A1 mRNA expressions were observed in the cells treated with IC-2-F. Protein expressions of α-SMA and Col1A1 caused by IC-2-F were also comparable to those caused by IC-2. Conclusion: IC-2-F was identified as a novel deactivating small-molecule compound for HSCs in vitro. These data suggest that IC-2-F is a promising medicine for liver fibrosis.
書誌情報 Yonago Acta Medica
en : Yonago Acta Medica

巻 63, 号 1, p. 79-87, 発行日 2020-02-20
雑誌内区分
値 Original Article
出版者
出版者 Tottori University Medical Press
ISSN
収録物識別子タイプ ISSN
収録物識別子 05135710
書誌レコードID
収録物識別子タイプ NCID
収録物識別子 AA00892882
DOI
関連タイプ isIdenticalTo
識別子タイプ DOI
関連識別子 10.33160/yam.2020.02.013
権利
権利情報 Yonago Acta medica 編集委員会
情報源
関連名称 Takuki Sakaguchi, Yohei Kono, Noriko Itaba, Minoru Morimoto, Hajime Isomoto, Goshi Shiota, Identification of a Novel Deactivating Small-Molecule Compound for Fibrogenic Hepatic Stellate Cells, Yonago Acta Medica, 2020, Volume 63, Issue 1, Pages 79-87, Rel
関連サイト
識別子タイプ URI
関連識別子 https://www.jstage.jst.go.jp/article/yam/63/1/63_2020.02.013/_article/
関連名称 https://www.jstage.jst.go.jp/article/yam/63/1/63_2020.02.013/_article/
関連サイト
識別子タイプ URI
関連識別子 http://www.lib.tottori-u.ac.jp/yam/yam/yam63-1/63-1contents.html
関連名称 http://www.lib.tottori-u.ac.jp/yam/yam/yam63-1/63-1contents.html
著者版フラグ
出版タイプ VoR
EISSN
値 1346-8049
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