| ○種別 (必須): | □ | 学術論文 (審査論文)
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| ○言語 (必須): | □ | 英語
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| ○著者 (必須): | 1. | 船本 雅文 ([徳島大学.大学院医歯薬学研究部.医学域.先端医学教育研究プロジェクト]/[徳島大学.大学院医歯薬学研究部.医学域.医科学部門.生理系.薬理学])
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| 2. | (英) Sunagawa Yoichi (日) (読)
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| 3. | (英) Gempei Mai (日) (読)
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| 4. | (英) Shimizu Kana (日) (読)
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| 5. | (英) Katanasaka Yasufumi (日) (読)
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| 6. | (英) Shimizu Satoshi (日) (読)
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| 7. | (英) Hamabe-Horiike Toshihide (日) (読)
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| 8. | (英) Appendino Giovanni (日) (読)
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| 9. | (英) Minassi Alberto (日) (読)
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| 10. | (英) Koeberle Andreas (日) (読)
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| 11. | (英) Komiyama Maki (日) (読)
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| 12. | (英) Mori Kiyoshi (日) (読)
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| 13. | (英) Hasegawa Koji (日) (読)
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| 14. | (英) Morimoto Tatsuya (日) (読)
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| ○題名 (必須): | □ | (英) Pyrazole-Curcumin Suppresses Cardiomyocyte Hypertrophy by Disrupting the CDK9/CyclinT1 Complex. (日)
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| ○要約 (任意): | □ | (英) The intrinsic histone acetyltransferase (HAT), p300, has an important role in the development and progression of heart failure. Curcumin (CUR), a natural p300-specific HAT inhibitor, suppresses hypertrophic responses and prevents deterioration of left-ventricular systolic function in heart-failure models. However, few structure-activity relationship studies on cardiomyocyte hypertrophy using CUR have been conducted. To evaluate if prenylated pyrazolo curcumin (PPC) and curcumin pyrazole (PyrC) can suppress cardiomyocyte hypertrophy, cultured cardiomyocytes were treated with CUR, PPC, or PyrC and then stimulated with phenylephrine (PE). PE-induced cardiomyocyte hypertrophy was inhibited by PyrC but not PPC at a lower concentration than CUR. Western blotting showed that PyrC suppressed PE-induced histone acetylation. However, an in vitro HAT assay showed that PyrC did not directly inhibit p300-HAT activity. As Cdk9 phosphorylates both RNA polymerase II and p300 and increases p300-HAT activity, the effects of CUR and PyrC on the kinase activity of Cdk9 were examined. Phosphorylation of p300 by Cdk9 was suppressed by PyrC. Immunoprecipitation-WB showed that PyrC inhibits Cdk9 binding to CyclinT1 in cultured cardiomyocytes. PyrC may prevent cardiomyocyte hypertrophic responses by indirectly suppressing both p300-HAT activity and RNA polymerase II transcription elongation activity via inhibition of Cdk9 kinase activity. (日)
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| ○キーワード (推奨): |
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| ○誌名 (必須): | □ | Pharmaceutics (Molecular Diversity Preservation International)
(pISSN: 1999-4923)
| ○ISSN (任意): | □ | 1999-4923
ISSN: 1999-4923
(eISSN: 1999-4923) Title: PharmaceuticsTitle(ISO): PharmaceuticsPublisher: Multidisciplinary Digital Publishing Institute (MDPI) (NLM Catalog)
(Scopus)
(CrossRef)
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| ○巻 (必須): | □ | 14
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| ○号 (必須): | □ | 6
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| ○頁 (必須): | □ | 1269 1269
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| ○年月日 (必須): | □ | 西暦 2022年 6月 15日 (令和 4年 6月 15日)
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| ○URL (任意): |
| ○DOI (任意): | □ | 10.3390/pharmaceutics14061269 (→Scopusで検索)
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| ○PMID (任意): | □ | 35745840 (→Scopusで検索)
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| ○備考 (任意): | 1. | (英) PublicationType: Journal Article (日)
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