摘要
酰基辅酶A-胆固醇酰基转移酶(ACAT)抑制剂是近年来降血脂和抗动脉粥样硬化药物研究的热点。两种全合成的药物在Ⅲ期临床试验被证明对动脉粥样硬化无效甚至有害,而天然抑制剂在结构上与合成抑制剂有很大的不同。筛选与研究天然抑制剂,作为药物设计的先导物,有可能开发出一些疗效显著的药物。本文综述了微生物来源的ACAT抑制剂的研究进展。
ACAT was viewed as potential therapeutic targets since the cholesterol-lowering and anti-atherosclerosis activity of its inhibitors. The synthetic drugs pactimibe and avasimibe proved inefficient in clinical trials. Nevertheless, natural inhibitors were structurally different. As lead compounds, they were expected to provide leads for drug design and development. The current status of studies on ACAT inhibitors from microorganisms was reviewed.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2011年第15期1418-1422,共5页
Chinese Journal of New Drugs
