| Item type |
文献 / Documents(1) |
| 公開日 |
2023-08-22 |
| アクセス権 |
|
|
アクセス権 |
open access |
| 資源タイプ |
|
|
資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
|
資源タイプ |
journal article |
| 出版社版DOI |
|
|
|
識別子タイプ |
DOI |
|
|
関連識別子 |
https://doi.org/10.3390/pharmaceutics14061269 |
|
|
言語 |
ja |
|
|
関連名称 |
10.3390/pharmaceutics14061269 |
| 出版タイプ |
|
|
出版タイプ |
VoR |
|
出版タイプResource |
http://purl.org/coar/version/c_970fb48d4fbd8a85 |
| タイトル |
|
|
タイトル |
Pyrazole-Curcumin Suppresses Cardiomyocyte Hypertrophy by Disrupting the CDK9/CyclinT1 Complex |
|
言語 |
en |
| 著者 |
船本, 雅文
スナガワ, ヨウイチ
ゲンペイ, マイ
シミズ, カナ
カタナサカ, ヤスフミ
シミズ, サトシ
ハマベ ホリイケ, トシヒデ
| ja |
ハマベ ホリイケ, トシヒデ
|
| ja-Kana |
ハマベ ホリイケ, トシヒデ
|
| en |
Hamabe-Horiike, Toshihide
|
Search repository
Appendino, Giovanni
Minassi, Alberto
Koeberle, Andreas
コミヤマ, マキ
モリ, キヨシ
ハセガワ, コウジ
モリモト, タツヤ
|
| 抄録 |
|
|
内容記述タイプ |
Abstract |
|
内容記述 |
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. |
|
言語 |
en |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
cardiomyocyte hypertrophy |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
p300 |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
curcumin |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
histone acetyltransferase |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
Cdk9 |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
主題 |
phosphorylation |
| 書誌情報 |
en : Pharmaceutics
巻 14,
号 6,
p. 1269,
発行日 2022-06-15
|
| 収録物ID |
|
|
収録物識別子タイプ |
ISSN |
|
収録物識別子 |
19994923 |
| 出版者 |
|
|
出版者 |
MDPI |
|
言語 |
en |
| 権利情報 |
|
|
言語 |
en |
|
権利情報 |
This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
| EID |
|
|
識別子 |
398899 |
|
識別子タイプ |
URI |
| 言語 |
|
|
言語 |
eng |
pharm_14_6_1269.pdf (2.38 MB)
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