Basic medicinal chemistry based on behavioral structure-building regulation of protein

基于蛋白质行为结构构建调控的基础药物化学

• 批准号: 24790119
• 负责人: AOYAMA hiroshi
• 金额: $ 2.75万
• 依托单位: Tokyo University of Pharmacy and Life Science
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2012
• 资助国家: 日本
• 起止时间: 2012-04-01 至 2014-03-31
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-24790119/
• 关键词: 虚血／再灌流障害; HCV; フォールディング; ダントロレン; 虚血・再灌流障害; ミトコンドリア; C型肝炎; 虚血性疾患; PTP

In this study, we tried to establish innovative drug development methodology by using a basic medicinal chemistry based on behavioral structure-building regulation of protein. A target of this study is folding regulatory factor, and illness to intend for both ischemia/reperfusion induced cell death and hepatitis C virus reproduction. As a result, we succeeded in development of compounds which have inhibitory effect of Ca2+-induced mitochondrial swelling. These compounds were considered to be capable of inhibitor for the ischemia/reperfusion induced cell death.

在这项研究中，我们试图通过使用基于蛋白质行为结构构建调控的基础药物化学来建立创新的药物开发方法学。这项研究的一个目标是折叠调节因子，并打算在疾病的同时导致缺血/再灌注诱导的细胞死亡和丙型肝炎病毒的复制。因此，我们成功地开发出了具有抑制钙离子诱导的线粒体肿胀作用的化合物。这些化合物被认为能够抑制缺血/再灌流所致的细胞死亡。

项目成果

Novel Strategy for Synthesis of Substituted Benzimidazo[1,2-a]quinolines

• DOI: 10.1021/ol4017723
• 发表时间: 2013-07-19
• 期刊: ORGANIC LETTERS
• 影响因子: 5.2
• 作者: Kato, Jun-ya;Ito, Yutaro;Yokomatsu, Tsutomu
• 通讯作者: Yokomatsu, Tsutomu

Small-molecular inhibitors of Ca2+-induced mitochondrial permeability transition (MPT) derived from muscle relaxant dantrolene

• DOI: 10.1016/j.bmc.2012.08.062
• 发表时间: 2012-11-01
• 期刊: BIOORGANIC & MEDICINAL CHEMISTRY
• 影响因子: 3.5
• 作者: Murasawa, Shinpei;Iuchi, Katsuya;Aoyama, Hiroshi
• 通讯作者: Aoyama, Hiroshi