HDL drug carriers for targeted therapy.
HDL drug carriers for targeted therapy.
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DOI：
10.1016/j.cca.2012.10.008
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发表时间：
2013-01
期刊：
影响因子：
--
通讯作者：
Xing Liu;Rong Suo;Shenglin Xiong;Qing-hai Zhang;G. Yi
中科院分区：
文献类型：
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作者：
Xing Liu;Rong Suo;Shenglin Xiong;Qing-hai Zhang;G. Yi
高密度脂蛋白胆固醇（HDL-C）的血浆浓度与心血管风险呈强负相关。HDL不是一种简单的脂质转运体，它含有特殊的蛋白质、信号脂质和microRNA，具有多种抗动脉粥样硬化活性。天然或重组HDL已成为将药物递送至特定靶点的潜在载体。然而，HDL的功能还取决于改变其结构和组成的酶，以及促进与微环境相互作用的细胞受体和膜微结构域。本文综述了体内增强HDL功能或靶向治疗的四种机制。第一个涉及小窝介导的HDL信号的募集以结合它们的受体。第二类是B I型清道夫受体（SR-BI），它介导HDL信号脂的锚定和流动性。第三个涉及卵磷脂-胆固醇酰基转移酶（LCAT）将信号脂质集中在HDL颗粒的表面。第四个是microRNAs（miRNAs）在血液中通过HDL传递到特定的靶点。对这四种机制的充分利用，将促进HDL携带靶向药物，提高HDL的临床应用价值。
Plasma concentrations of high-density lipoprotein cholesterol (HDL-C) are strongly and inversely associated with cardiovascular risk. HDL is not a simple lipid transporter, but possesses multiple anti-atherosclerosis activities because it contains special proteins, signaling lipid, and microRNAs. Natural or recombinant HDLs have emerged as potential carriers for delivering a drug to a specified target. However, HDL function also depends on enzymes that alter its structure and composition, as well as cellular receptors and membrane micro-domains that facilitate interactions with the microenvironment. In this review, four mechanisms predicted to enhance functions or targeted therapy of HDL in vivo are discussed. The first involves caveolae-mediated recruitment of HDL signal to bind their receptors. The second involves scavenger receptor class B type I (SR-BI) mediating anchoring and fluidity for signal-lipid of HDL. The third involves lecithin-cholesterol acyltransferase (LCAT) concentrating the signaling lipid at the surface of the HDL particle. The fourth involves microRNAs (miRNAs) being delivered in the blood to special targets by HDL. Exploitation of these four mechanisms will promote HDL to carry targeted drugs and increase HDL's clinical value.