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Fragment-based drug discovery for the sweet tooth of prostate cancer

Fragment-based drug discovery for the sweet tooth of prostate cancer
针对前列腺癌的基于片段的药物发现
批准号:
2755856
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:
2022
资助国家:
英国
项目状态:
未结题
起止时间:
2022 至 --

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中文摘要
翻译
八分之一的男性在一生中会患上前列腺癌,这使得改善治疗方案成为绝对必要。改变的糖结构,也称为聚糖,是前列腺癌的一个一致特征,但在药物发现中却大大不足。最近,我们已经确定了一种糖基化酶作为一种新的治疗靶点,并为开发更好的前列腺癌治疗方法提供了令人兴奋的机会。该项目由英国前列腺癌和化学生物学研究所共同资助,将专注于基于片段的药物发现,靶向这种酶。我们将联合收割机结合新的化学空间和建模方法,以产生具有合适相互作用特征的先导化合物。将进行生物学评估,以设想一种药物,击中糖基化,甜食的前列腺癌。我们正在寻找具有强大的化学背景的申请人,最好在药物发现/药物化学方面有一定的经验。您将领导一个合作项目,需要与PI协调,记录保存和可重复,安全的实验室工作的奉献精神的优秀技能。该项目将在伦敦帝国理工学院全新的分子科学研究中心进行,该中心是英国化学科学的旗舰,拥有最先进的实验室空间和设备。它的特点是与合作者在纽卡斯尔和萨拉戈萨(西班牙)的工作,以及在伦敦市中心的弗朗西斯克里克研究所借调的潜力。
英文摘要
One in eight men get prostate cancer in their lifetime, making improved therapy options an absolute necessity. Altered sugar structures, also called glycans, are a consistent feature of prostate cancer but are vastly underexplored in drug discovery. Very recently, we have identified a glycosylation enzyme as a novel therapeutic target and an exciting opportunity to develop better treatments for prostate cancer. This project, co-funded by Prostate Cancer UK and the Institute of Chemical Biology, will focus on fragment-based drug discovery target this enzyme. We will combine newly-available chemical space and modelling approaches to generate lead compounds with suitable interaction profiles. Biological evaluation will be performed to envisage a drug that hits glycosylation, the sweet tooth of prostate cancer. We are looking for applicants with a strong background in chemistry, ideally with some experience in drug discovery/medicinal chemistry. You will be leading a collaborative project, requiring excellent skills in coordinating with PIs, record-keeping and dedication for reproducible, safe laboratory work. This project will be carried out at the brand-new Molecular Sciences Research Hub at Imperial College London, a flagship of chemical sciences in the UK with state-of-the-art laboratory space and equipment. It features work with collaborators in Newcastle and Zaragoza (Spain), as well as the potential for a secondment at the Francis Crick Institute in central London.
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