Identification and optimisation of small molecule inhibitors of APP1 as novel therapeutics.
Identification and optimisation of small molecule inhibitors of APP1 as novel therapeutics.
APP1 小分子抑制剂的鉴定和优化作为新型疗法。
批准号：
2108967
负责人：
金额：
$0.0万
依托单位：
依托单位国家：
英国
项目类别：
Studentship
财政年份：
2018
资助国家：
英国
项目状态：
已结题
起止时间：
2018 至 --
中文摘要
翻译
本提案的目的是确定有效的、可溶的和细胞可渗透的化学工具作为APP的抑制剂，其具有进一步验证抑制机制和进一步开发成治疗药物的潜力。我们的策略是利用APP的高分辨率结构，在计算合理的命中验证练习，开发有效的和细胞渗透性抑制剂。其目标是产生可以进一步开发成治疗剂的铅样化学探针。
英文摘要
The objective of this proposal will be to identify potent, soluble and cell permeable chemical tools as inhibitors of APP with potential to further validate the mechanism of inhibition and for further development into a therapeutic drug. Our strategy is to exploit the high-resolution structure of APP in a computational rational hit validation exercise to develop potent and cell permeable inhibitors. The aim will be to generate lead-like chemical probes that can be further developed into therapeutic agents.
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