『徳島大学 教育・研究者情報データベース (EDB)』---[学外] /
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種別 (必須): 学術論文 (審査論文) [継承]
言語 (必須): 英語 [継承]
招待 (推奨):
審査 (推奨): Peer Review [継承]
カテゴリ (推奨): 研究 [継承]
共著種別 (推奨): 国際共著 (徳島大学内研究者と国外研究機関所属研究者との共同研究) [継承]
学究種別 (推奨):
組織 (推奨): 1.徳島大学.大学院社会産業理工学研究部.生物資源産業学域 (2017年4月1日〜) [継承]
著者 (必須): 1. (英) Ahn Mok-Ryeon (日) (読)
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2. (英) Bae Ji-Yeon (日) (読)
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[継承]
3. (英) Jeong Da-Hye (日) (読)
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[継承]
4. (英) Takahashi Hideaki (日) 髙橋 秀明 (読) たかはし ひであき
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学籍番号 (推奨): **** [ユーザ]
[継承]
5.宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座])
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[継承]
6. (英) Maruta Hiroshi (日) (読)
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[継承]
題名 (必須): (英) Both triazolyl ester of ketorolac (15K) and YM155 inhibit the embryonic angiogenesis in ovo (fertilized eggs) via their common PAK1-survivin/VEGF signaling pathway.  (日)    [継承]
副題 (任意):
要約 (任意): (英) 15 K is 1,2, 3-triazolyl ester of ketorolac, an old pain-killer, that blocks PAK1 by its R-form and inhibits COX-2 by its S-form. Mainly due to a robust increase in cell-permeability, 15K is over 500 times more potent than ketorolac in both anti-cancer and anti-PAK1 activities in cell culture with IC50 around 24 nM. However, 15K has no anti-AKT activity. Angiogenesis requires at least the kinase PAK1, and perhaps the kinase AKT as well, and is essential for a robust growth of solid tumors. Thus, in this study, we examined the potential antiangiogenic activity of 15K both in ovo and cell culture, prior to its in vivo (xenograft) anti-cancer activity test. The IC50 of 15K against the embryonic angiogenesis in ovo in CAM (chorioallantoic membrane) assay is around 1 nmol/egg. Surprizingly, however, 15K failed to inhibit the tube formation of HUVECs (human umbilical vein endothelial cells) in cell culture even at high as 150 μM. In an attempt to solve this mystery, we tested both in ovo as well as HUVECs-based anti-angiogenic activity of a potent survivin-suppressor called YM155, which blocks PAK1, in addition to AKT. YM155 is slightly more potent than 15K in CAM assay with IC50 around 0.5 nmol/egg, and apparenty inhibits the tube formation of HUVECs with IC50 around 18 nM. According to a few previous findings with the direct PAK1-inhibitor frondoside A (FRA), the tube formation of HUVECs depends solely on PAK1. Thus, the failure of 15K to affect their tube formation is most likely due to their drug (15K)-resistance. Furthermore, unlike FRA, YM155 killed HUVECs with IC50 around 18 nM, clearly indicating that AKT is essential for survival of HUVECs, instead of their tube formation.  (日)    [継承]
キーワード (推奨): 1. (英) HUVECs (日) (読) [継承]
2. (英) PAK1 (日) (読) [継承]
3. (英) YM155 (日) (読) [継承]
4.血管新生 (angiogenesis) [継承]
5. (英) ketorolac ester (15K) (日) (読) [継承]
6. (英) survivin suppressor (日) (読) [継承]
発行所 (推奨):
誌名 (必須): Drug Discoveries & Therapeutics (Shandong da xue zhong ri yao wu shai xuan zhongxin/International Advancement Center for Medicine & Health Research)
(pISSN: 1881-7831, eISSN: 1881-784X)

ISSN (任意): 1881-7831
ISSN: 1881-7831 (pISSN: 1881-7831, eISSN: 1881-784X)
Title: Drug discoveries & therapeutics
Title(ISO): Drug Discov Ther
Supplier: 特定非営利活動法人 バイオ&ソーシャル・サイエンス推進国際研究交流会
Publisher: International Advancement Center for Medicine & Health Research Co., Ltd. (IACMHR Co., Ltd.)
 (NLM Catalog  (医中誌Web  (J-STAGE  (Scopus  (CrossRef (Scopus information is found. [need login])
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(必須): 11 [継承]
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(必須): 300 306 [継承]
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年月日 (必須): 西暦 2018年 1月 12日 (平成 30年 1月 12日) [継承]
URL (任意):
DOI (任意): 10.5582/ddt.2017.01058    (→Scopusで検索) [継承]
PMID (任意): 29332887    (→Scopusで検索) [継承]
NAID (任意): 130006308126 [継承]
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被引用数 (任意):
指導教員 (推奨): 1.宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座]) [継承]
備考 (任意): 1.(英) Article.ELocationID: 10.5582/ddt.2017.01058  (日)    [継承]
2.(英) Article.PublicationTypeList.PublicationType: Journal Article  (日)    [継承]
3.(英) KeywordList.Keyword: HUVECs  (日)    [継承]
4.(英) KeywordList.Keyword: PAK1  (日)    [継承]
5.(英) KeywordList.Keyword: YM155  (日)    [継承]
6.(英) KeywordList.Keyword: angiogenesis  (日)    [継承]
7.(英) KeywordList.Keyword: ketorolac ester (15K)  (日)    [継承]
8.(英) KeywordList.Keyword: survivin suppressor  (日)    [継承]

標準的な表示

和文冊子 ● Mok-Ryeon Ahn, Ji-Yeon Bae, Da-Hye Jeong, Hideaki Takahashi, Yoshihiro Uto and Hiroshi Maruta : Both triazolyl ester of ketorolac (15K) and YM155 inhibit the embryonic angiogenesis in ovo (fertilized eggs) via their common PAK1-survivin/VEGF signaling pathway., Drug Discoveries & Therapeutics, Vol.11, No.6, 300-306, 2018.
欧文冊子 ● Mok-Ryeon Ahn, Ji-Yeon Bae, Da-Hye Jeong, Hideaki Takahashi, Yoshihiro Uto and Hiroshi Maruta : Both triazolyl ester of ketorolac (15K) and YM155 inhibit the embryonic angiogenesis in ovo (fertilized eggs) via their common PAK1-survivin/VEGF signaling pathway., Drug Discoveries & Therapeutics, Vol.11, No.6, 300-306, 2018.

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