Development of the artificial transcription factor which promotes endogenous gene expression in cell

促进细胞内源基因表达的人工转录因子的开发

• 批准号: 22750151
• 负责人: SHIMOGAWA Hiroki
• 金额: $ 2.66万
• 依托单位: Kyoto University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2010
• 资助国家: 日本
• 起止时间: 2010 至 2011
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-22750151/
• 关键词: レンチノロール; 転写因子; 転写活性化; 小分子有機化合物; 細胞膜透過性; Sur2; アダマンタン; iPS細胞

The wrenchnolol analogue was developed, it has improved water solubility and with lower molecule weight.The compound 10 which reported have transcriptional activation ability was synthesized, and this compound was assayed by transcriptional activation assay using streptavidin-biotin system. As the result, by this system, the compound 10 did not show transcriptional activation ability.The transcriptional activation ability of the compound 10 was measured using glucocorticoid receptor-dexamethasone system. By this system, the compound 10 also did not show transcriptional activation ability.

开发了水溶性更好、分子量更小的双羟萘洛尔类似物，合成了具有转录激活活性的化合物10，并利用链霉亲和素-生物素系统对该化合物进行了转录激活活性检测。其结果是，在该系统中，化合物10没有表现出转录激活能力，使用糖皮质激素受体-地塞米松系统测定化合物10的转录激活能力。通过该系统，化合物10也没有显示转录激活能力。

项目成果

Mitochondorial surface-specific fluorescent probe activated by bioconversion.

通过生物转化激活线粒体表面特异性荧光探针。

• 发表时间: 2011
• 期刊: Angew.Chem.Int.Ed.
• 作者: Yoshinori Kawazoe;Hiroki Shimogawa;Ayato Sato;Motonari Uesugi.
• 通讯作者: Motonari Uesugi.

Chemical library screening identifies a small moleculethat downregulates SOD1 transcription for drugs to treat ALS.

化学库筛选发现了一种下调 SOD1 转录的小分子，可用于治疗 ALS 的药物。

• 发表时间: 2011
• 期刊: The Journal of Biomolecular Screening
• 作者: Murakami G;Inoue H;Tsukita K;Asai Y;Amagai Y;Aiba K;Shimogawa H;Uesugi M;Nakatsuji N;Takahashi R.
• 通讯作者: Takahashi R.

Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.

• DOI: 10.1021/jm200304y
• 发表时间: 2011-07-14
• 期刊: Journal of medicinal chemistry
• 影响因子: 7.3
• 作者: Kamisuki S;Shirakawa T;Kugimiya A;Abu-Elheiga L;Choo HY;Yamada K;Shimogawa H;Wakil SJ;Uesugi M
• 通讯作者: Uesugi M

細胞形態変化誘導活性を指標としたアクチン阻害化合物の探索

以细胞形态变化诱导活性为指标，寻找肌动蛋白抑制化合物

• 发表时间: 2010
• 作者: 住谷瑛理子;下川浩輝;佐々木宏明;小鹿一;末永聖武;上杉志成
• 通讯作者: 上杉志成

Cell-Morphology Profiling of a Natural Product Library Identifies Bisebromoamide and Miuraenamide A as Actin Filament Stabilizers

• DOI: 10.1021/cb1003459
• 发表时间: 2011-05-01
• 期刊: ACS CHEMICAL BIOLOGY
• 影响因子: 4
• 作者: Sumiya, Eriko;Shimogawa, Hiroki;Uesugi, Motonari
• 通讯作者: Uesugi, Motonari