Selective PROTACS against PDE5 + PDE7 as novel treatments for CNS disorders and cancer

针对 PDE5 PDE7 的选择性 PROTACS 作为中枢神经系统疾病和癌症的新疗法

• 批准号: 2893294
• 金额: --
• 依托单位: University of Glasgow
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2022
• 资助国家: 英国
• 起止时间: 2022 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2893294
• 关键词: Selective; PROTACS; against; PDE5; PDE7

Studentship strategic priority area: Industrial collaborative researchKeywords: PROTACs, phosphodiesterasesAbstract: This project will focus on testing and optimising PDE5 and PDE7 isoform selective PROTACS that could be used as novel treatments for CNS disorders and cancer. PDE5 and PDE7 PROTACs will be tested in cell lines to determine successful knockdown of PDE5 and PDE7 and establish selectivity of PROTACs towards specific PDE isoforms. Molecular Modelling techniques will be used to visualise PROTAC-target interaction and inform drug structure optimisation. Furthermore, bioinformatic analysis will help detect dysregulation of PDE5 and PDE7 isoforms in other diseases that could be amenable to PDE5/PDE7 PROTAC drug development and treatment.

学生战略优先领域：产业合作研究关键词：PROTAC，磷酸二酯酶摘要：本项目将重点测试和优化PDE5和PDE7亚型选择性PROTAC，它们可以作为治疗中枢神经系统疾病和癌症的新药物。PDE5和PDE7 PROTAC将在细胞系中进行测试，以确定PDE5和PDE7的成功敲除，并建立PROTAC对特定PDE亚型的选择性。分子建模技术将被用来可视化PROTAC-目标相互作用，并为药物结构优化提供信息。此外，生物信息学分析将有助于检测其他疾病中PDE5和PDE7亚型的失调，这些疾病可能适用于PDE5/PDE7 PROTAC药物开发和治疗。