LIBRARIES OF AMINOGLYCOSIDES AND MIMETICS TARGETING RNA

靶向 RNA 的氨基糖苷和模拟物文库

• 批准号: 6269919
• 负责人: C H WONG
• 金额: $ 16.38万
• 依托单位: SCRIPPS RESEARCH INSTITUTE, THE
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-05-07 至 1999-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6269919
• 关键词: RNA; aminoglycoside antibiotics; angiogenesis inhibitors; antineoplastics; antisense nucleic acid; chemical registry /resource; chemical synthesis; drug design /synthesis /production; drug resistance; drug screening /evaluation; guanosine; inhibitor /antagonist; integrins; phosphoric ester; surface plasmon resonance

Libraries of aminoglycosides and mimetics targeting RNA This project will take rational and combinatorial approaches to develop aminoglycosides and mimetics targeting cancer-associated RNA as well as angiogenesis. It will focus on the following programs: 1. We have discovered that 1,3-hydroxyamines are better than the guanidine groups as recognition motif for the complexation of phosphodiesters and the Hoogsteen face of guanosine in RNA. We will use this new motif as a core to develop small-molecule libraries to screen for inhibitors (using surface plasmon resonance) targeting RNAs and integrins associated with cancer and angiogenesis. 2. Attachment of reactive groups or short antisense deoxyoligonucleotides to the lead candidates to develop sequence selective RNA cleaving agents. Significant contributions in the areas of biomedicine, drug design, drug resistance, synthetic organic chemistry and the discovery of a new generation of anti-cancer agents are expected.

靶向 RNA 的氨基糖苷类和模拟物文库 本项目将采取合理、组合的方式进行开发 靶向癌症相关 RNA 的氨基糖苷类和模拟物以及 血管生成。它将重点关注以下计划： 1.我们发现1,3-羟胺比胍更好 基团作为磷酸二酯络合的识别基序和 RNA 中鸟苷的 Hoogsteen 面。我们将使用这个新主题作为 开发小分子库来筛选抑制剂的核心（使用 表面等离子共振）靶向与相关的RNA和整合素 癌症和血管生成。 2. 连接反应基团或短反义脱氧寡核苷酸 开发序列选择性 RNA 切割剂的主要候选者。 在生物医学、药物设计、药物研究等领域做出了重大贡献 电阻、合成有机化学和新发现 预计抗癌药物的产生。