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Development of novel 191Pt-labeled Hoechst33258: 191Pt is more suitable than 111In for targeting DNA
https://repo.qst.go.jp/records/86115
https://repo.qst.go.jp/records/86115feedef2a-b54f-4f78-8a5e-cdec6922e0a2
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2022-04-07 | |||||
タイトル | ||||||
タイトル | Development of novel 191Pt-labeled Hoechst33258: 191Pt is more suitable than 111In for targeting DNA | |||||
言語 | ||||||
言語 | eng | |||||
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 | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Honoka, Obata
× Honoka, Obata× Atsushi, Tsuji× Katsushi, Kumata× Hitomi, Sudo× Katsuyuki, Minegishi× Kotaro, Nagatsu× Hideo, Takakura× Mikako, Ogawa× Akihiro, Kurimasa× Zhang, Ming-Rong× Honoka, Obata× Atsushi, Tsuji× Katsushi, Kumata× Hitomi, Sudo× Katsuyuki, Minegishi× Kotaro, Nagatsu× Mikako, Ogawa× Zhang, Ming-Rong |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Abstract: This study aims to establish new labeling methods for no-carrier–added radio-Pt (191Pt) and to evaluate the in vitro properties of 191Pt-labeled agents compared with those of agents labeled with the common emitter 111In. 191Pt was complexed with the DNA-targeting dye Hoechst33258 via diethylenetriaminepentaacetic acid (DTPA) or the sulfur-containing amino acid cysteine (Cys). The intranuclear fractions of 191Pt- and 111In-labeled Hoechst33258 were comparable, indicating that the labeling for 191Pt via DTPA or Cys and the labeling for 111In via DTPA worked equally well. 191Pt showed a DNA-binding/cellular uptake ratio more than one order of magnitude greater than that of 111In. [191Pt]Pt-Hoechst33258 labeled via Cys showed a higher cellular uptake than that labeled via DTPA, resulting in a very high DNA-binding fraction of [191Pt]Pt-Cys-Hoechst33258 and extensive DNA damage. Our labeling methods of radio-Pt, especially via Cys, promote the development of radio-Pt-based agents for use in Auger electron therapy targeting DNA. |
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書誌情報 |
Journal of Medicinal Chemistry 巻 65, 号 7, p. 5690-5700, 発行日 2022-03 |
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出版者 | ||||||
出版者 | ACS Publications | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0022-2623 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1021/acs.jmedchem.1c02209 | |||||
関連サイト | ||||||
識別子タイプ | URI | |||||
関連識別子 | https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c02209 |