NOVEL STRATEGY FOR BIOSUBSTRATE PROTEIN KINASE INHIBITOR

生物底物蛋白激酶抑制剂的新策略

• 批准号: 2793639
• 负责人: PAUL G GROTHAUS
• 金额: $ 11.41万
• 依托单位: HAWAII BIOTECH, INC.
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-04-13 至 2000-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2793639
• 关键词: chemical registry /resource; combinatorial chemistry; enzyme inhibitors; enzyme substrate; protein kinase; protein tyrosine kinase

DESCRIPTION (Adapted from the application): Protein kinases play key roles in many cell signaling pathways, and enhanced activity of the protein kinases has been implicated in cancer and other proliferative diseases. Specific inhibitors would allow selective regulation of cell growth mechanisms and therefore, may be potentially useful cancer therapeutics. The overall goal of this project is to discover new classes of potent and specific inhibitors of individual serine/threonine and tyrosine protein kinases. The applicant proposes to approach this problem with a two-pronged combinatorial, transition state analog strategy to develop highly potent bisubstrate inhibitors. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE

描述（改编自应用程序）：蛋白激酶在以下方面发挥关键作用： 许多细胞信号传导途径，以及蛋白激酶活性的增强， 与癌症和其他增殖性疾病有关。特异性抑制剂 可以选择性地调节细胞生长机制，因此， 是潜在有用的癌症治疗剂。该项目的总体目标是 发现新的种类的有效的和特异性的个体抑制剂， 丝氨酸/苏氨酸和酪氨酸蛋白激酶。申请人建议 我用一个双管齐下的组合过渡态类似物来解决这个问题 开发高效双底物抑制剂的策略。 拟议商业应用：不可用