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

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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.