Development of medicinal molecules having biologically functions targeting the PI3K/Akt pathway and the TGF-b/Smad pathway
Development of medicinal molecules having biologically functions targeting the PI3K/Akt pathway and the TGF-b/Smad pathway
批准号:
23390028
负责人:
OTSUKA Masami
金额:
$11.56万
依托单位:
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (B)
财政年份:
2011
资助国家:
日本
项目状态:
已结题
起止时间:
2011-04-01 至 2014-03-31
中文摘要
本研究旨在设计和合成PI3K/Akt通路的激活剂和TGF-b/Smad通路的抑制剂,开发调节这两种通路串扰的药物。针对PI3K/Akt通路,合成了包含磷酸肌醇和二酰基甘油部分的化合物。以TGF-b/Smad通路为靶点,合成了含有吡啶和金属结合侧链的化合物。这些化合物可以作为脑保护剂、糖尿病、癌症、癌症转移和硬皮病的药物。
英文摘要
The present study aimed at the design and synthesis of activators of the PI3K/Akt pathway and inhibitors of the TGF-b/Smad pathway to develop drugs to regulate the crosstalk of the two pathways. Targeting the PI3K/Akt pathway, compounds comprising inositol phosphate and diacyl glycerol moiety were synthesized. Targeting the TGF-b/Smad pathway, compounds comprising the pyridine and metal-binding side chains were synthesized. These compounds could be useful as brain-protecting agents, drugs for diabetes, cancer, cancer metastasis, and scleroderma.
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Design and synthesis of biotinylated inositol 1,3,4,5-tetrakisphosphate targeting Grp1 Pleckstrin Homogy domain
靶向 Grp1 Pleckstrin 同源结构域的生物素化肌醇 1,3,4,5-四磷酸的设计与合成
DOI:
--
发表时间:
2011
期刊:
Bioorg.Med.Chem.
影响因子:
--
作者:
[中村優希, 國安明彦, 安楽健作]
通讯作者:
安楽健作
PHドメインタンパク質に結合し膜に移動させるmyo-イノシトール誘導体の合成
与 PH 结构域蛋白结合并易位至膜的肌醇衍生物的合成
DOI:
--
发表时间:
2012
期刊:
影响因子:
--
作者:
[筑葉晃一, 工藤康太, 舛田岳史, 安楽健作, 大塚雅巳]
通讯作者:
大塚雅巳
ペプチド性新規DNA切断分子の設計と合成
新型肽DNA切割分子的设计与合成
DOI:
--
发表时间:
2013
期刊:
影响因子:
--
作者:
[井田智弓,岡本良成,藤田美歌子,黒崎博雅,大塚雅巳]
通讯作者:
井田智弓,岡本良成,藤田美歌子,黒崎博雅,大塚雅巳
HIV-1 MA蛋白質と強く結合するイノシトールリン脂質誘導体の合成と評価
与HIV-1 MA蛋白强结合的肌醇磷脂衍生物的合成与评价
DOI:
--
发表时间:
2013
期刊:
影响因子:
--
作者:
[安楽健作, 立石大, 古賀涼子, 東大志, 本山敬一, 有馬英俊, 大塚雅巳, 藤田美歌子]
通讯作者:
藤田美歌子
熊本大学大学院薬学教育部分子機能薬学専攻分子機能薬学講座生体機能分子合成学分野
熊本大学药学研究生院、分子功能药学系、分子功能药学系、生物功能性分子合成系
DOI:
--
发表时间:
期刊:
影响因子:
--
作者:
[]
通讯作者:
共 34 条
Design and synthesis of anti-brain tumor and brain-protective drugs using brain-targeting peptides
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批准号:24659048
-
项目类别:Grant-in-Aid for Challenging Exploratory Research
-
资助金额:$2.41万
-
财政年份:2012
-
负责人:OTSUKA Masami
-
依托单位:
Design and synthesis of anti-HIV agents that inhibit the Vif-mediated proteasome degradation of APOBEC3G
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批准号:22659024
-
项目类别:Grant-in-Aid for Challenging Exploratory Research
-
资助金额:$1.89万
-
财政年份:2010
-
负责人:OTSUKA Masami
-
依托单位:
Design of DNA-cleaving and -crosslinking agents based on NFκB and HMGA proteins aiming at the application to cancer therapy
-
批准号:20390033
-
项目类别:Grant-in-Aid for Scientific Research (B)
-
资助金额:$12.15万
-
财政年份:2008
-
负责人:OTSUKA Masami
-
依托单位:
Development of zinc chelators with protein specificity aiming at molecular target therapy of cancer
-
批准号:17390030
-
项目类别:Grant-in-Aid for Scientific Research (B)
-
资助金额:$10.12万
-
财政年份:2005
-
负责人:OTSUKA Masami
-
依托单位:
Molecular design of anti-AIDS drugs targeting the viral and host zinc proteins
-
批准号:15390038
-
项目类别:Grant-in-Aid for Scientific Research (B)
-
资助金额:$8.51万
-
财政年份:2003
-
负责人:OTSUKA Masami
-
依托单位:
Molecular design of anti-AIDS drugs targeting the human transcription machinery employed for the replication of AIDS virus
-
批准号:12557219
-
项目类别:Grant-in-Aid for Scientific Research (B)
-
资助金额:$7.49万
-
财政年份:2000
-
负责人:OTSUKA Masami
-
依托单位:
Molecular Design of Ras Farnesyltransferase Inhibitors
-
批准号:11694297
-
项目类别:Grant-in-Aid for Scientific Research (B)
-
资助金额:$5.82万
-
财政年份:1999
-
负责人:OTSUKA Masami
-
依托单位:
Development of compounds for multiple regulation of intracellular signaling
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批准号:11470496
-
项目类别:Grant-in-Aid for Scientific Research (B).
-
资助金额:$4.22万
-
财政年份:1999
-
负责人:OTSUKA Masami
-
依托单位:
Molecular design and synthesis of anti-cancer compounds that cause apoptosis
-
批准号:09672280
-
项目类别:Grant-in-Aid for Scientific Research (C)
-
资助金额:$2.3万
-
财政年份:1997
-
负责人:OTSUKA Masami
-
依托单位: