PH-Responsive Micelles for Controlled Enzyme Inhibitor Release

用于控制酶抑制剂释放的 PH 响应胶束

• 批准号: 2671072
• 金额: --
• 依托单位: Durham University
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2021
• 资助国家: 英国
• 起止时间: 2021 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2671072
• 关键词: PH; Responsive; Micelles; Controlled; Enzyme

In this project, we will design pH-responsive micelles, loaded with the anticancer agent SAHA, to target effective drug deliver at the tumour site. The histone-deacetylase enzymes (HDACs) are an important class of molecular targets in cancer therapy, due to their role in gene expression and cancer metastasis. SAHA is a HDAC inhibitor used to treat T-cell lymphoma. Despite its benefits, SAHA has been shown to have off-target effects, including potential genotoxicity. In this project, we will produce delivery systems for SAHA that lead to active molecule only at the tumour. To selectively deliver the drug to the tumour, we will develop micelles that release the SAHA at the lower pH and more reducing environment of the tumour compared to the typical extracellular environment. The project comprises inhibitor synthesis, micelle synthesis, micelle analysis and biological testing.

在这个项目中，我们将设计pH响应胶束，装载抗癌剂SAHA，靶向有效的药物输送在肿瘤部位。组蛋白去乙酰化酶（HDAC）由于其在基因表达和癌症转移中的作用而成为癌症治疗中的一类重要分子靶标。SAHA是用于治疗T细胞淋巴瘤的HDAC抑制剂。尽管SAHA有好处，但已被证明具有脱靶效应，包括潜在的遗传毒性。在这个项目中，我们将生产SAHA的输送系统，只在肿瘤处产生活性分子。为了选择性地将药物递送至肿瘤，我们将开发胶束，其与典型的细胞外环境相比在较低的pH和肿瘤的更还原的环境下释放SAHA。该项目包括抑制剂合成、胶束合成、胶束分析和生物测试。