論文 - 詳細
| RRC ID | 64803 |
|---|---|
| 著者 | Yonezawa H, Sugawara A, Sakyo T, Uehara Y, Kawano T, Nishiya N. |
| タイトル | IMU1003, an atrarate derivative, inhibits Wnt/β-catenin signaling. |
| ジャーナル | Biochem Biophys Res Commun |
| Abstract |
Aberrant activation of the canonical Wnt/β-catenin signaling pathway triggers tumorigenesis in various tissues. This study identified an atrarate compound, IMU14, derived from filamentous fungi as an inhibitor of Wnt/β-catenin signaling in phenotypic chemical inhibitor screening of the zebrafish eyeless phenotype. Its derivatization resulted in synthesis of IMU1003 with enhanced Wnt inhibitory activity. IMU1003 inhibited β-catenin/TCF-dependent transcriptional activation and decreased nuclear β-catenin level. In addition, IMU1003 selectively decreased viability and target gene products of the Wnt/β-catenin signaling pathway in human non-colorectal cancer cell lines harboring intact APC and β-catenin. Therefore, atrarate derivatives inhibit Wnt/β-catenin signaling and show anticancer potential, and we developed a new class of chemical backbones for Wnt/β-catenin signaling inhibitors. |
| 巻・号 | 532(3) |
| ページ | 440-445 |
| 公開日 | 2020-11-12 |
| DOI | 10.1016/j.bbrc.2020.08.031 |
| PII | S0006-291X(20)31588-6 |
| PMID | 32891433 |
| MeSH | Animals Animals, Genetically Modified Antineoplastic Agents / pharmacology Cell Line, Tumor Cell Proliferation / drug effects Cell Survival / drug effects Down-Regulation / drug effects Drug Screening Assays, Antitumor Gene Expression / drug effects HEK293 Cells Humans Hydroxybenzoates / pharmacology* Mutation Wnt Signaling Pathway / drug effects* Wnt Signaling Pathway / genetics Zebrafish / embryology Zebrafish / genetics beta Catenin / metabolism* |
| IF | 2.985 |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | X(Twitter) |
| 各媒体での言及数の合計 | 1 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ゼブラフィッシュ | RIKEN WT |