論文 - 詳細
| RRC ID | 42755 |
|---|---|
| 著者 | Sasaki S, Bando T, Minoshima M, Shimizu T, Shinohara K, Takaoka T, Sugiyama H. |
| タイトル | Sequence-specific alkylation of double-strand human telomere repeat sequence by pyrrole-imidazole polyamides with indole linkers. |
| ジャーナル | J Am Chem Soc |
| Abstract |
We designed and synthesized pyrrole (Py)-imidazole (Im) hairpin polyamide 1-(chloromethyl)-5-hydroxy-1,2-dihydro-3H-benz[e]indole (seco-CBI) conjugates 1 and 2, which target both strands of the double-stranded region of the human telomere repeat sequences, 5'-d(TTAGGG)(n)-3'/5'-d(CCCTAA)(n)-3'. High-resolution denaturing polyacrylamide gel electrophoresis demonstrated that conjugates 1 and 2 alkylated DNA at the 3' A of 5'-ACCCTA-3' and 5'-AGGGTTA-3', respectively. Cytotoxicities of conjugates 1 and 2 were evaluated using 39 human cancer cell lines; averages of log IC(50) values for conjugates 1 and 2 were -6.96 (110 nM) and -7.24 (57.5 nM), respectively. Conjugates 1 and 2 have potential as antitumor drugs capable of targeting telomere repeat sequence. |
| 巻・号 | 128(37) |
| ページ | 12162-8 |
| 公開日 | 2006-9-20 |
| DOI | 10.1021/ja0626584 |
| PMID | 16967966 |
| MeSH | Alkylation Antineoplastic Agents / chemical synthesis Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology Base Sequence Cell Line, Tumor Electrophoresis, Polyacrylamide Gel Humans Indoles / chemical synthesis Indoles / chemistry* Indoles / pharmacology* Molecular Sequence Data Neoplasms / genetics Neoplasms / metabolism Pyrroles / chemical synthesis Pyrroles / chemistry* Pyrroles / pharmacology* Repetitive Sequences, Nucleic Acid Substrate Specificity Telomere / chemistry Telomere / genetics Telomere / metabolism* |
| IF | 14.612 |
| 引用数 | 28 |
| WOS 分野 | CHEMISTRY, MULTIDISCIPLINARY |
| 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 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 2 |
| 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 | |
| ヒト・動物細胞 | MRC-5 NHSF46(RCB0162) |