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药物化学与靶点确证

药物化学与靶点确证
  • 导航:首页 > 科学基金
  • 批准号:81622043
  • 批准年度: 2016年
  • 学科分类:合成药物化学(H3001) |
  • 项目负责人:梁广
  • 负责人职称:研究员
  • 依托单位:温州医科大学
  • 资助金额:130万元
  • 项目类别:优秀青年科学基金项目
  • 研究期限:2017年01月01日 至 2019年12月31日
  • 中文关键词: 药物化学;靶点;确证
  • 英文关键词:Medicinal Chemistry;Target validation;Chemical biology;Inflammation;Anti-cancer drug

项目摘要

中文摘要

如何发现和确证重要靶标蛋白质及其先导化合物是药物化学领域的重要科学问题之一。申请人利用基于已知结构的药物化学,结合化学生物学和药理学,从事炎症与肿瘤相关疾病的活性小分子药物设计、新药发现和新靶点确证研究,利用这种“药物化学+靶点确证”的小分子创新药物研究模式,以期促进我国新靶标、新机制和新结构的first-in-class药物研究与开发。.已发现13个新的先导化合物,4个新化合物作为候选一类新药进入临床前研究,并为急慢性炎症和肿瘤疾病发现确证了4个重要的有效靶点。.申请人已主持国家自然基金3 项和863 课题1 项;申请国际PCT 专利2 项,获得国家发明专利授权9项。自2011年1月至今,以通讯作者发表SCI论文53篇,合计IF=247,其中中科院JCR分区一区论文11篇,二区论文24篇。论文合计被他引861 次,单篇最高他引119次,2015年申请人以第一完成人获教育部自然科学二等奖。

英文摘要

To find and validate key protein targets as well as their leading structures is the key scientific problem in the field of medicinal chemistry. Wiith an interdisciplinary knowledge background, the applicant combined medicinal chemistry and pharmacology in his research. Based on the known active molecules and targeting inflammation-related diseases and cancers, Dr Liang performed his studies including small-molecule drug design, new drug discovery, and new target validation. Taking the research strategy of “medicinal chemistry plus target validation”, he is looking forward to contribute to the Chinese first-in-class drug research and development..In the past several years, he discovered 13 new leading compounds and 4 new candidates which are in preclinical studies, as well as validated 4 new protein targets for the treatment of inflammatory and cancer diseases..So far, Dr Liang has already assumed three NSFC grants and one national 863 project, and obtained 9 authorized Chinese invention patents. Since 2011, he published 53 peer-reviewed articles or reviews as the corresponding author in international SCI journals, including 4 papers in J Med Chem, 1 paper in Diabetes, and 5 papers in Oncotarget. His papers have been cited for a total of 861 times. The most cited one has been cited for 119 times. In 2015, one of his research projects was awarded by the Ministry of Education, China.

评估说明

    国家自然科学基金项目“药物化学与靶点确证”发布于爱科学iikx,并永久归类于相关科学基金导航中,仅供广大科研工作者查询、学习、选题参考。国科金是根据国家发展科学技术的方针、政策和规划,以及科学技术发展方向,面向全国资助基础研究和应用研究,发挥着促进我国基础研究源头创新的作用。国科金的真正价值在于它能否为科学进步和社会发展带来积极的影响。

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