Characterisation of the molecular structure and function of topoisomerase I using anticancer agents as molecular probes acting in a new allosteric binding-site

使用抗癌剂作为作用于新变构结合位点的分子探针表征拓扑异构酶 I 的分子结构和功能

• 批准号: RGPIN-2016-05069
• 负责人: Fortin, Sébastien
• 金额: $ 1.82万
• 依托单位: Université Laval
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2017
• 资助国家: 加拿大
• 起止时间: 2017-01-01 至 2018-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=632842
• 关键词: Characterisation; molecular; structure; function; topoisomerase

Topoisomerases (Topo) are important therapeutic targets to treat many cancers. To that end, inhibitors of these enzymes are amongst the most widely used anticancer drugs. For example, Topo I is an enzyme essential to maintain the integrity of our genetic code to avoid introducing harmful mutations while inhibitors of these enzymes induce breakages of this code and death of the cells. I have developed for nearly two years as an independent researcher a new family of promising anticancer drugs referred to “

拓扑异构酶(Topo)是治疗多种癌症的重要靶点。为此，这些酶的抑制剂是使用最广泛的抗癌药物之一。例如，Topo I是一种维持我们遗传密码的完整性以避免引入有害突变所必需的酶，而这些酶的抑制剂则会导致密码的破坏和细胞的死亡。作为一名独立研究员，我已经开发了近两年的时间，开发了一系列有前途的抗癌药物，