Identifying deubiquitylating enzymes (DUBs) as targets for treating of platinum-resistant ovarian cancer

确定去泛素化酶（DUB）作为治疗铂耐药性卵巢癌的靶标

• 批准号: 131062
• 金额: $ 18.35万
• 依托单位: MISSION THERAPEUTICS LTD
• 依托单位国家: 英国
• 项目类别: Feasibility Studies
• 财政年份: 2013
• 资助国家: 英国
• 起止时间: 2013 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=131062
• 关键词: Identifying; deubiquitylating; enzymes; DUBs; targets

Novel therapies tailored for treatment of platinum-resistant ovarian cancer is an area of clear unmet need. Ovarian cancer is responsible for more deaths per year than any other cancer of the female reproductive system and developing drug resistance remains the main limitation of current chemotherapies. We propose an innovative approach to identifying novel drug targets for drug-resistant ovarian cancer that would exploit the very changes in the tumour that have led to the resistance. We propose to do this by screening all known human deubiquitylases (DUBs) – a novel, druggable class of enzymes – to identify innovative targets whose inhibition would selectively kill or re-sensitise drug-resistant ovarian tumours. The best validated targets will then enter the MISSION Therapeutics Ltd pipeline for further drug discovery efforts with a view to new, innovative and effective chemotherapies entering the clinic.

为铂类耐药卵巢癌的治疗量身定制的新疗法是一个明显未满足需求的领域。卵巢癌每年造成的死亡人数比任何其他女性生殖系统癌症都多，耐药性的发展仍然是目前化疗的主要限制。我们提出了一种创新的方法来确定耐药卵巢癌的新药物靶点，该方法将利用导致耐药性的肿瘤变化。我们建议通过筛选所有已知的人类去泛素化酶（DUB）-一种新型的，可药物化的酶-来确定创新的靶点，其抑制将选择性地杀死或重新敏感耐药卵巢肿瘤。最好的验证目标将进入使命Therapeutics Ltd管道，以进一步进行药物发现工作，以期新的，创新的和有效的化疗进入临床。