甾醇O-酰基转移酶
化学
甾醇
酰基转移酶
生物化学
胆固醇
酶
同工酶
药理学
医学
脂蛋白
作者
Pinaki Bhattacharjee,Nicholas Rutland,Malliga R. Iyer
标识
DOI:10.1021/acs.jmedchem.2c01265
摘要
Sterol O-acyltransferase (SOAT) is a membrane-bound enzyme that aids the esterification of cholesterol and fatty acids to cholesterol esters. SOAT has been studied extensively as a potential drug target, since its inhibition can serve as an alternative to statin therapy. Two SOAT isozymes that have discrete functions in the human body, namely, SOAT1 and SOAT2, have been characterized. Over three decades of research has focused on candidate SOAT1 inhibitors with unsatisfactory results in clinical trials. Recent research has focused on targeting SOAT2 selectively. In this perspective, we summarize the literature covering various SOAT inhibitory agents and discuss the design, structural requirements, and mode of action of SOAT inhibitors.
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