Project/Area Number |
02557084
|
Research Category |
Grant-in-Aid for Developmental Scientific Research (B)
|
Allocation Type | Single-year Grants |
Research Field |
Chemical pharmacy
|
Research Institution | Univ. of Tokyo |
Principal Investigator |
SHUDO Koichi Univ. Tokyo, Prof., 薬学部, 教授 (50012612)
|
Co-Investigator(Kenkyū-buntansha) |
KAGECHIKA Hiroyuki Univ. Tokyo Assist Prof., 薬学部, 助手 (20177348)
OHWADA Tomohiko Univ. Tokyo, Assist Prof., 薬学部, 助手 (20177025)
橋本 祐一 東京大学, 応微研, 助教授 (90164798)
遠藤 泰之 東京大学, 薬学部, 講師 (80126002)
|
Project Period (FY) |
1990 – 1992
|
Project Status |
Completed (Fiscal Year 1992)
|
Budget Amount *help |
¥12,900,000 (Direct Cost: ¥12,900,000)
Fiscal Year 1992: ¥3,700,000 (Direct Cost: ¥3,700,000)
Fiscal Year 1991: ¥4,400,000 (Direct Cost: ¥4,400,000)
Fiscal Year 1990: ¥4,800,000 (Direct Cost: ¥4,800,000)
|
Keywords | retinoid / vitamin A / retinoic acid / retinoid antagonist / cancer / leukemia / differentiation / retinoid receptor / 分化 / レチノイドレセプタ- / 分子設計 / HL60 / 核レセプタ- / ビタミンA酸 / 形態形成 / 癌治療 / シリコン |
Research Abstract |
Molecular design ant synthesis of retinoids were practiced toward possible therapeutic applications. 1. New retinoids containing a trimethylsilyl or trimethylgermyl moiety were prepared. Some of them are very stong in the differentiation inducing bioassay. 2. Trans amide conformation of some synthetic retinoids is proved more important for the strong biological activity. 3. Retinoid receptors were expressed in animal cells and also in E. Coli. Using these receptors binding constants of several synthetic retinoids were evaluated. 4. Fluorescent retinoid probes were prepared. 5. Retinoid antagonists were synthesized for the first time. 6. An in vitro cancerstatic activity was tested using a malignant transformation model. 7. Three retinoid symposiums were held during the term, where some of the results were presented.
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