2011 Fiscal Year Final Research Report
Development of novel molecular-targeted medicine against aminopeptidase
| Project/Area Number |
21390373
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Digestive surgery
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| Research Institution | The University of Tokyo |
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Principal Investigator |
KARAKO Takashi (TANG Wei) 東京大学, 医学部附属病院, 助教 (00313213)
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| Co-Investigator(Kenkyū-buntansha) |
KOKUDO Norihiro 東京大学, 医学部附属病院, 教授 (00205361)
SEKIMIZU Kazuhisa 東京大学, 薬学系研究科, 教授 (90126095)
NAKATA Munehiro 東海大学, 工学部, 教授 (00266371)
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| Project Period (FY) |
2009 – 2011
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| Keywords | 分子標的治療薬 / 肝細胞癌 / 浸潤 / APN / 血管新生 |
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| Research Abstract |
This study was aimed to develop novel inhibitors of aminopeptidase N(APN) overexpressed on cancer cell membrane and to evaluate the suppressive effect on cancer cell growth and angiogenesis. A newly-synthesized compound 24F, one of hydroxamic acid derivatives, inhibited the activity of aminopeptidases expressed on HL60 cell membrane. This compound inhibited the growth and invasion of hepatoma cell lines. In addition, incubation of vascular endothelial cells with 24F was found to be effective for the suppression of the angiogenic phenomena such as migration and tube formation. Furthermore, a newly-synthesized bestatin derivative LYP also had the ability to inhibit cancer cell growth as well as migration and tube formation of vascular endothelial cells. These results suggest that newly-synthesized aminopeptidase inhibitors are effective as an anti-cancer agent for hepatoma via inhibition of cancer cell invasion and angiogenesis surrounding cancer tissue.
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[Journal Article] LYP, a novel bestatin derivative, inhibits cell growth and suppressesAPN/CD13 activity in human ovariancarcinoma cells more potently thanbestatin2011
Author(s)
Gao JJ, Gao ZH, Zhao CR, Yuan Y, Cui SX, Zhang XF, Cheng YN, Xu WF, Tang W, Qu XJ.
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Journal Title
Invest New Drugs
Volume: 29(4)
Pages: 574-582
DOI
Peer Reviewed
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[Journal Article] KL-6mucin in metastatic liver cancertissues from primary colorectalcarcinoma2009
Author(s)
Zhang K, Tang W, Qu X, Guo Q, InagakiY, Seyama Y, Abe H, Gai R, Kokudo N, Sugawara Y, Nakata M, Makuuchi M. Y, Seyama Y, Abe H, Gai R, Kokudo N, Sugawara Y, Nakata M
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Journal Title
KL-6mucin in metastatic liver cancertissues from primary colorectalcarcinoma.
Volume: 56(93)
Pages: 960-963
Peer Reviewed
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[Journal Article] Clinicopathology of sialomucin : MUC1, particularly KL-6 mucin, ingastrointestinal, hepatic andpancreatic cancers2009
Author(s)
Inagaki Y, Xu H, Nakata M, Seyama Y, Hasegawa K, Sugawara Y, Tang W, KokudoN.
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Journal Title
Biosci Trends
Volume: 3(6)
Pages: 220-232
URL
Peer Reviewed
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