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Requirement of the 8-hydroxyl group in the 5-chloro-8-quinolinol for its Action as a Radioprotective Agonist
https://repo.qst.go.jp/records/72229
https://repo.qst.go.jp/records/722294035f5fd-ee12-4382-9a36-6ee147e00e07
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-03-22 | |||||
| タイトル | ||||||
| タイトル | Requirement of the 8-hydroxyl group in the 5-chloro-8-quinolinol for its Action as a Radioprotective Agonist | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Ujita, Shohei
× Ujita, Shohei× Mmorita, Akinori× Aoki, Shin× Nishi, Yurie× Tatsuro, Teraoka× Sasatani, Megumi× Wang, Bing× Takahashi, Ippei× Tanaka, Kaoru× Yamakawa, Tomoaki× Nenoi, Mitsuru× Kamiya, Kenji× Inaba, Toshiya× 王 冰× 田中 薫× 根井 充 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Development of radioprotectors is a very important strategy for reducing radiation risk. We have explored compounds that target a zinc-binding site (ZBS) in p53 , and found that 5-chloro-8-quinolinol (5CHQ) has a unique p53-agonistic activity that shifts its transactivation from proapoptotic to protective responses including the enhancement of p21 induction and the suppression of PUMA induction. The dose-reduction factors of 5CHQ in total-body and abdominally irradiated mice were about 1.2 and 1.3, respectively. In this study, in order to investigate the hydroxyl group at the 8-position of the quinolone ring of 5CHO in its radioprotective function, we synthesized 5-chloro-8-methoxyquinoline (5CMQ), whose 8-hydroxyl group is methylated, and comfirmed that it had no antiapoptotic activity against p-53-dependent apoptosis in 10Gy-irradiated MOLT-4 cells when assessed by Annexin V-FITC staining. In addition, immunoblotting analysis revealed that 5CMQ did not alter the expression of P53 and the products of two p53-target genes, p21 and PUMA, These data indicate that the 8-hydroxyl group of 5CHQ is required for its metal-chelating activity in suppressing apoptosis and shifting p-53-transactivation. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 「第1回国際シンポジウム」「Scientific Underpinning for Restoration from a Radiation Disaster（放射線災害からの復興を支える科学的基盤）」 | |||||
| 発表年月日 | ||||||
| 日付 | 2017-02-22 | |||||
| 日付タイプ | Issued | |||||
