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General Review Article

脂肪酸合酶抑制剂的结构和生物活性

卷 26, 期 39, 2019

页: [7081 - 7101] 页: 21

弟呕挨: 10.2174/0929867326666190507105022

价格: $65

摘要

背景：脂肪酸合酶（FAS或FASN）是一种重要的酶，可催化长链脂肪酸的从头合成。最近有许多研究报道，FAS是发现抗肥胖和抗癌药物的共同目标。人们对寻找新型FAS抑制剂产生了极大的兴趣，并导致了200多种抑制剂的报道。方法：收集有关FAS抑制剂的研究文献，并通过Web of Science和PubMed等主要数据库进行分析。然后总结了所有这些已报道的FAS抑制剂的化学结构，FAS抑制活性和结构-活性关系（SAR）。结果：在过去20年中已报道的248种FAS抑制剂，根据其结构特点，可分为硫代内酯，丁内酯和丁内酰胺，多酚，生物碱，萜类化合物和其他结构。并提出了每种类型的高抑制结构的SAR。结论：在所报道的FAS抑制剂中，一系列合成的喹啉酮衍生物表现出最强的抑制活性。食品和草药中存在的天然多酚由于其安全性和有效性而在医学探索中显示出更大的适应性。此外，从微生物和海洋天然产物中筛选FAS抑制剂可能是未来的热门研究方向。

关键词: 脂肪酸合酶（FAS），抑制剂，结构，抑制活性，构效关系（SAR），抗肥胖，抗癌。

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