Targeting Sterol O-Acyltransferase/Acyl-CoA:Cholesterol Acyltransferase (ACAT): A Perspective on Small-Molecule Inhibitors and Their Therapeutic Potential,Journal of Medicinal Chemistry

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Targeting Sterol O-Acyltransferase/Acyl-CoA:Cholesterol Acyltransferase (ACAT): A Perspective on Small-Molecule Inhibitors and Their Therapeutic Potential
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-12-06 , DOI: 10.1021/acs.jmedchem.2c01265
Pinaki Bhattacharjee ₁ , Nicholas Rutland ₁ , Malliga R Iyer ₁

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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.

中文翻译：

靶向甾醇 O-酰基转移酶/酰基辅酶 A：胆固醇酰基转移酶 (ACAT)：小分子抑制剂及其治疗潜力的展望

甾醇O -酰基转移酶 (SOAT) 是一种膜结合酶，有助于将胆固醇和脂肪酸酯化为胆固醇酯。SOAT 作为潜在的药物靶标已被广泛研究，因为它的抑制作用可以作为他汀类药物治疗的替代品。已经表征了在人体中具有离散功能的两种 SOAT 同工酶，即 SOAT1 和 SOAT2。超过三十年的研究集中在候选 SOAT1 抑制剂上，但在临床试验中结果不尽如人意。最近的研究集中于选择性地靶向 SOAT2。从这个角度来看，我们总结了涵盖各种 SOAT 抑制剂的文献，并讨论了 SOAT 抑制剂的设计、结构要求和作用方式。

更新日期：2022-12-06

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