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| ファイル | 記述 | サイズ | フォーマット | |
|---|---|---|---|---|
| chem.202004421.pdf | 3.18 MB | Adobe PDF | 見る/開く |
| タイトル: | Evaluation of the DNA Alkylation Properties of a Chlorambucil‐Conjugated Cyclic Pyrrole‐Imidazole Polyamide |
| 著者: | Hirose, Yuki Hashiya, Kaori Bando, Toshikazu  Sugiyama, Hiroshi   https://orcid.org/0000-0001-8923-5946 (unconfirmed) |
| 著者名の別形: | 廣瀬, 優希 橋谷, かおり 板東, 俊和 杉山, 弘 |
| キーワード: | alkylation antitumor agents DNA alkylator DNA recognition drug delivery |
| 発行日: | Feb-2021 |
| 出版者: | Wiley |
| 誌名: | Chemistry - A European Journal |
| 巻: | 27 |
| 号: | 8 |
| 開始ページ: | 2782 |
| 終了ページ: | 2788 |
| 抄録: | Hairpin pyrrole-imidazole polyamides (hPIPs) and their chlorambucil (Chb) conjugates (hPIP-Chbs) can alkylate DNA in a sequence-specific manner, and have been studied as anticancer drugs. Here, we conjugated Chb to a cyclic PIP (cPIP), which is known to have a higher binding affinity than the corresponding hPIP, and investigated the DNA alkylation properties of the resulting cPIP-Chb using the optimized capillary electrophoresis method and conventional HPLC product analysis. cPIP-Chb conjugate 3 showed higher alkylation activity at its binding sites than did hPIP-Chb conjugates 1 and 2. Subsequent HPLC analysis revealed that the alkylation site of conjugate 3, which was identified by capillary electrophoresis, was reliable and that conjugate 3 alkylates the N3 position of adenine as do hPIP-Chbs. Moreover, conjugate 3 showed higher cytotoxicity against LNCaP prostate cancer cells than did conjugate 1 and cytotoxicity comparable to that of conjugate 2. These results suggest that cPIP-Chbs could be novel DNA alkylating anticancer drugs. |
| 著作権等: | This is the peer reviewed version of the following article:[Chemistry - A European Journal, 27(8), 2782-2788], which has been published in final form at https://doi.org/10.1002/chem.202004421. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions. This article may not be enhanced, enriched or otherwise transformed into a derivative work, without express permission from Wiley or by statutory rights under applicable legislation. Copyright notices must not be removed, obscured or modified. The article must be linked to Wiley’s version of record on Wiley Online Library and any embedding, framing or otherwise making available the article or pages thereof by third parties from platforms, services and websites other than Wiley Online Library must be prohibited. The full-text file will be made open to the public on 14 January 2022 in accordance with publisher's 'Terms and Conditions for Self-Archiving'. This is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 |
| URI: | http://hdl.handle.net/2433/268789 |
| DOI(出版社版): | 10.1002/chem.202004421 |
| PubMed ID: | 33145851 |
| 出現コレクション: | 学術雑誌掲載論文等 |
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