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载脂蛋白A-I模拟物

Apolipoprotein A-I mimetics.

作者信息

Reddy Srinivasa T, Navab Mohamad, Anantharamaiah Gattadahalli M, Fogelman Alan M

机构信息

aDepartment of Medicine bDepartment of Obstetrics and Gynecology cDepartment of Molecular and Medical Pharmacology, David Geffen School of Medicine at UCLA, Los Angeles, California dDepartment of Medicine, University of Alabama at Birmingham, Alabama USA.

出版信息

Curr Opin Lipidol. 2014 Aug;25(4):304-8. doi: 10.1097/MOL.0000000000000092.

Abstract

PURPOSE OF REVIEW

To summarize recent publications in the field of apolipoprotein mimetics.

RECENT FINDINGS

Apolipoprotein mimetic peptides continue to show efficacy in a number of animal models of disease and demonstrate properties that make them attractive as potential therapeutic agents. A number of new apolipoprotein mimetics have been described recently. A major site of action of apolipoprotein mimetic peptides was found to be in the small intestine in which they decrease the levels of proinflammatory bioactive lipids. A major problem related to the use of apolipoprotein mimetic peptides is their cost, particularly those that need to be generated by solid phase synthesis with chemical addition of end-blocking groups. Novel approaches to apolipoprotein mimetic therapy have emerged recently that show promise in overcoming these barriers.

SUMMARY

Despite the recent failure of therapies designed to raise HDL-cholesterol in humans, an approach to therapy using mimetics of HDL and its components continues to show promise.

摘要

综述目的

总结载脂蛋白模拟物领域的近期出版物。

最新发现

载脂蛋白模拟肽在多种疾病动物模型中持续显示出疗效,并展现出使其成为潜在治疗药物的吸引力的特性。最近描述了一些新的载脂蛋白模拟物。发现载脂蛋白模拟肽的一个主要作用部位是小肠,它们在小肠中可降低促炎生物活性脂质的水平。与使用载脂蛋白模拟肽相关的一个主要问题是其成本,特别是那些需要通过固相合成并化学添加封端基团来制备的肽。最近出现了载脂蛋白模拟物治疗的新方法,有望克服这些障碍。

总结

尽管最近旨在提高人类高密度脂蛋白胆固醇的疗法失败了,但使用高密度脂蛋白及其成分模拟物的治疗方法仍显示出前景。

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