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首页> 外文期刊>Biochemical Pharmacology >Cholesteryl ester transfer protein facilitates the movement of water-insoluble drugs between lipoproteins: a novel biological function for a well-characterized lipid transfer protein.
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Cholesteryl ester transfer protein facilitates the movement of water-insoluble drugs between lipoproteins: a novel biological function for a well-characterized lipid transfer protein.

机译：胆固醇酯转移蛋白可促进水不溶性药物在脂蛋白之间的移动：脂类转移蛋白的新型生物学功能。

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摘要

This review article addresses the recently discovered finding that cholesteryl ester transfer protein (CETP) can facilitate the transfer of water-insoluble drugs between different lipoprotein subclasses. This protein, which is often referred to as lipid transfer protein I (LTP I), is involved in the lipid regulation of lipoproteins. It is responsible for the facilitated transfer of core lipoprotein lipids, cholesteryl ester and triglycerides, and approximately one-third of the coat lipoprotein lipid, phosphatidylcholine, between different plasma lipoproteins. The human body appears to recognize exogenous water-insoluble drugs as lipid-like particles, which suggests that these compounds may interact with lipoproteins just like endogenous plasma lipids, and thus their transfer between lipoproteins may be facilitated by plasma CETP. Patients with a variety of diseases (i.e. diabetes, cancer, AIDS) often exhibit hypo- and/or hypercholesterolemia and triglyceridemia, commonly referred to as dyslipidemias, which result in changes in their plasma lipoprotein-lipid composition and concentration. The interaction of water-insoluble drugs with these dyslipidemic lipoproteins may be responsible for the differences seen in the pharmacokinetics and pharmacodynamics of the drug within different diseased patient populations. It is possible that these differences may be linked to the ability of CETP to transfer these compounds from one lipoprotein to another. This review examines the current understanding of the relationship between CETP activity and the lipoprotein distribution of a number of compounds (e.g. amphotericin B and cyclosporine A). It further suggests that additional research will expand our understanding of the role of CETP to explain other functions in lipophilic drug distribution and metabolism.
机译：这篇评论文章解决了最近发现的发现，胆固醇酯转移蛋白（CETP）可以促进不同脂蛋白亚类之间水不溶性药物的转移。该蛋白通常称为脂质转移蛋白I（LTP I），与脂蛋白的脂质调节有关。它负责促进核心脂蛋白脂质，胆固醇酯和甘油三酸酯以及大约三分之一的外壳脂蛋白脂质，磷脂酰胆碱在不同血浆脂蛋白之间的转移。人体似乎将外源性水不溶性药物识别为脂质样颗粒，这表明这些化合物可能像脂蛋白一样与内源性血浆脂质相互作用，因此血浆CETP可以促进它们在脂蛋白之间的转移。患有多种疾病（例如糖尿病，癌症，艾滋病）的患者通常表现出低胆固醇和/或高胆固醇血症和甘油三酸酯血症，通常称为血脂异常，导致血浆脂蛋白-脂质组成和浓度发生变化。水不溶性药物与这些血脂异常脂蛋白的相互作用可能是造成该药物在不同患病人群中药代动力学和药效学差异的原因。这些差异可能与CETP将这些化合物从一种脂蛋白转移到另一种脂蛋白的能力有关。这篇综述检查了对CETP活性与许多化合物（例如两性霉素B和环孢霉素A）脂蛋白分布之间关系的当前理解。它进一步表明，其他研究将扩大我们对CETP的作用的理解，以解释亲脂性药物分布和代谢中的其他功能。

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