2012 Fiscal Year Final Research Report
Search for the anti-tumor derivatives containing the somatostatin sequence focusing on the hydrophobic index
| Project/Area Number |
22590111
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kobe Gakuin University |
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Principal Investigator |
TSUDA Yuko 神戸学院大学, 薬学部, 教授 (10098478)
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| Co-Investigator(Kenkyū-buntansha) |
MIZUSHINA Yoshiyuki 神戸学院大学, 栄養学部, 准教授 (20307705)
MIYAZAKI Anna 神戸学院大学, 薬学部, 助教 (00340919)
YOKOI Toshio 神戸学院大学, 薬学部, 教授 (50122255)
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| Project Period (FY) |
2010 – 2012
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| Keywords | 抗腫瘍活性 / 疎水性 / ソマトスタチン配列 / DNA polymerase 阻害 |
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| Research Abstract |
A structure-activity relationship studies revealed that hydrophobicity of YO-14 could be responsible for their antiproliferative activity. Thishypothesis has been explored in this project using the somatostatin sequence,X-TyrD-Trp-Y, and peptide synthesis technique: (1) substitution of Tyr produced morehydrophobic YO compounds with higher antiproliferative activity than YO-14;(2) double replacement (X-Tyr-Ile-NH-aphthalene) created a potent and ss -specific DNA polinhibitor; (3)the distribution of YO compounds incorporated fluorescent NBD, demonstrated that an adamantane moiety had an excellent permeability.
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[Journal Article] Plasmin inhibitor reduces T-cell lymphoid tumor growth by suppressing matrix matalliproteinase-9-dependent CD11b+/F4/80+ myeloid cell recruitment.2012
Author(s)
Ishihara M., Nishida C., Tashiro Y., Critli I., Rosenkvist J., Koizumi M., Okaji Y., Yamamoto R., Yagita H., Okumura K., Nishikori M., Wanaka K., Tsuda Y., Okada Y., Nakauchi H., Heissig B., Hattori K.
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Journal Title
Leukemia.
Volume: 26
Pages: 332-339
DOI
Peer Reviewed
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[Journal Article] Synthesis and anticancer activities of lipophilic somatostatin derivatives. Peptide2012; Proceedings of the 32nd European Peptide Symposium, Edited by Kokotos2012
Author(s)
Imazumi H., Suyama T., Takami D., Hidaka K., Miyazaki A., Yokoi T., Kuriyama I., Yoshida H., Mizushina Y., Tsuda Y.
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Journal Title
G., et al.
Pages: 666-667
URL
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[Presentation] Synthesis and anticancer activities of lipophilic somatostatin derivatives.2012
Author(s)
Inazumi H., Suyama T., Takami D., Hidaka K., Miyazaki A., Yokoi T., Kuriyama I., Yoshida H., Mizushina Y., Tsuda Y.
Organizer
The 32nd European Peptide Symposium
Place of Presentation
Athens, Greece
Year and Date
20120900
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