SAR studies to validate novel Fatty Acid Synthase (FASN) inhibitors as anti-cancer therapeutics

脂肪酸合成酶（FASN）已被证明是癌症的关键治疗靶点。大多数正常细胞从饮食中获取脂肪酸，因此不需要或表达FASN。相比之下，许多类型的癌细胞表达高水平的FASN，这种表达与患者预后不良有关。Sareum发现了一系列新的FASN抑制剂，能够阻止癌细胞增殖。这项可行性研究的目的是研究这些抑制剂的化学修饰是否可以提高它们的效力和稳定性，从而保证在一个完整的先导优化计划中投资，以开发用于患者临床试验的候选分子。

The enzyme Fatty Acid Synthase (FASN) has been shown to be a key therapeutic target in cancer. Most normal cells acquire fatty acids from diet, so do not require or express FASN. By contrast, many types of cancer cell express high levels of FASN, and this expression is associated with poor patient prognosis. Sareum has discovered a novel series of inhibitors of FASN that are able to prevent cancer cell proliferation. The aim of this feasibility study is to investigate whether chemical modification of these inhibitors can improve their potency and stability, and thus warrant the investment in a full lead optimisation programme to develop candidate molecules for clinical trials in patients.