既存薬剤を用いたPKM2活性剤の探索と癌治療への早期応用戦略

Material type: 文書・図像類

Author: 玉田, 真由美ほか

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Publication date: 2014

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Note (General)：: type:text近年, pyruvate kinase M2(PKM2)が癌特有な好気性解糖の制御因子であり, その活性剤が抗癌効果をもつ可能性が報告されている。過去に報告した如く(Tamada et al., Cancer Res 2012), PKM2活性上昇は, 間接的に癌の糖消費抑制を誘導...

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科研費研究者番号 : 80528133

科研費研究者番号 : 80264282

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Material Type: 文書・図像類
Title: 既存薬剤を用いたPKM2活性剤の探索と癌治療への早期応用戦略
Author/Editor: 玉田, 真由美
佐谷, 秀行
Author Heading: 玉田, 真由美
佐谷, 秀行
Publication Date: 2014
Publication Date (W3CDTF): 2014
Alternative Title: キソンヤクザイオモチイタ PKM2 カッセイザイノタンサクトガンチリョウエノソウキオウヨウセンリャク
Kison yakuzai o mochiita PKM2 kasseizai no tansaku to gan chiryo eno soki oyo senryaku
The applied strategic research for the sake of cancer treatment ; the discovery of puruvate kinase M2 (PKM2) activator out of existing drugs
Periodical title: 科学研究費補助金研究成果報告書
Text Language Code: jpn
eng
Subject Heading: 癌,糖代謝,pyruvate kinase M2,代謝変動,既存薬
Target Audience: 一般
Note (General): type:text
近年, pyruvate kinase M2(PKM2)が癌特有な好気性解糖の制御因子であり, その活性剤が抗癌効果をもつ可能性が報告されている。過去に報告した如く(Tamada et al., Cancer Res 2012), PKM2活性上昇は, 間接的に癌の糖消費抑制を誘導することから, 糖消費抑制するものにはPKM2活性剤が含まれると考え, 当研究室構築の既存薬ライブラリーを使用し, 糖消費・解糖系最終産物の乳酸産生抑制・PKM2チロシンリン酸化抑制を評価し, PKM2活性剤候補を選別した。酵素活性測定, 解糖系から正常細胞が主に利用するミトコンドリア呼吸への代謝変動, 抗癌効果の評価も進行中である。 Recently, PKM2 has been reported to be one of the most important factors to maintain glycolic phenotype which is the unique character of cancer. Thus, the possibility of PKM2 activator as an anti-cancerous drug has attracted attention. We investigated to discover PKM2 activator, which induce the metabolic shift from aerobic glycolysis to mitochondrial respiration mainly used by normal cells, out of existing drugs. We examined whether there was the drug which inhibits glucose consumption, lactate production, and tyrosine phosphorylation of PKM2 out of existing drugs, based on our idea that PKM2 activator may be included in the drugs which inhibit glucose consumption.We have already found some candidate drugs, and advance examination such as measurement of PKM2 enzyme activity, metabolic shift, and anti-cancerous effect.
研究種目 : 若手研究(B) 研究期間 : 2013～2014 課題番号 : 25870717 研究分野 : 癌の代謝
Access Restrictions: 限定公開
Related Material: 科研費研究者番号 : 80528133
科研費研究者番号 : 80264282
Data Provider (Database): 国立情報学研究所 : 学術機関リポジトリデータベース（IRDB）（機関リポジトリ）
https://irdb.nii.ac.jp
Original Data Provider (Database): 慶應義塾大学 : 慶應義塾大学学術情報リポジトリ