Project/Area Number |
22590111
|
Research Category |
Grant-in-Aid for Scientific Research (C)
|
Allocation Type | Single-year Grants |
Section | 一般 |
Research Field |
Drug development chemistry
|
Research Institution | Kobe Gakuin University |
Principal Investigator |
TSUDA Yuko 神戸学院大学, 薬学部, 教授 (10098478)
|
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)
|
Project Period (FY) |
2010 – 2012
|
Project Status |
Completed (Fiscal Year 2012)
|
Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2011: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2010: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
|
Keywords | 抗腫瘍活性 / 疎水性 / ソマトスタチン配列 / DNA polymerase 阻害 / DNA polymerase阻害 |
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.
|