Potentiation of Topoisomerase I Inhibitors

拓扑异构酶 I 抑制剂的增强作用

• 批准号: 6481388
• 负责人: Jing-Zhen Deng
• 金额: $ 10万
• 依托单位: PINNACLE PHARMACEUTICALS
• 依托单位国家: 美国
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-04-01 至 2003-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6481388
• 关键词: DNA topoisomerases; antineoplastics; biological products; biological response modifiers; cell free system; drug design /synthesis /production; drug discovery /isolation; enzyme inhibitors; method development; tissue /cell culture; yeasts

DESCRIPTION (provided by applicant): The overall goal of this SBIR is the identification of small molecules that can reinforce the antitumor activity of DNA topoisomerase I inhibitors by acting at a biochemical locus linked functionally to topoisomerase I. This is to be done by selecting natural products from plant and marine extracts that inhibit the topoisomerase I-linked locus, and then modifying the structures of the isolated active principles. The compounds so identified will be evaluated in cell free systems, and in suitable yeast tester strains and mammalian cell lines. Optimized inhibitors will be evaluated in suitable animal tumor models as potentiators of the activity of DNA topoisomerase I inhibitors. PROPOSED COMMERCIAL APPLICATION: The goal of this program is the identification and commercialization of agents that can potentiate the activity of topisomerase I inhibitors as antitumor agents. The annual market for an agents. The annual market for an agent of this type should be well in excess of $100 million.

描述（由申请人提供）：此SBIR的总体目标是 鉴定可以增强抗肿瘤活性的小分子 DNA拓扑异构酶I抑制剂通过在链接的生化基因座作用 从功能上到拓扑异构酶。这是通过选择天然来完成的 抑制拓扑异构酶I连接的植物和海洋提取物的产品 基因座，然后修改孤立的活动原理的结构。这 如此确定的化合物将在无细胞系统中评估，并在合适的 酵母测试仪菌株和哺乳动物细胞系。优化的抑制剂将是 在合适的动物肿瘤模型中评估是 DNA拓扑异构酶I抑制剂。 拟议的商业应用： 该程序的目的是鉴定和商业化可以增强拓扑酶I抑制剂作为抗肿瘤剂的活性的药物。 代理商的年度市场。 这种类型代理商的年度市场应超过1亿美元。