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ABCA1 agonist peptides for the treatment of disease

机译：ABCA1激动剂多肽，用于治疗疾病

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Purpose of reviewThe review summarizes information pertaining to the preclinical development of new apolipoprotein (apo) E mimetic peptides that stimulate cellular cholesterol efflux.Recent findingsSmall -helical peptides based on the C-terminal domain of apoE have been developed for therapeutic applications. These peptides stimulate cellular cholesterol efflux via the ATP-binding cassette transporter A1 (ABCA1) with high potency, like native apolipoproteins on a molar basis. This potent activity has been related to the unique ability of these peptides to maintain -helix structure upon dilution. Recent structure-activity studies improving the safety features of these mimetic peptides have greatly improved their potential for clinical use. These studies have identified structural features of the class A -helix motif that induce muscle toxicity and hypertriglyceridemia, which may have implications for the design of other HDL mimetic peptides.SummaryABCA1 is an integral membrane protein that plays a central role in biology. Its principal function is to mediate the efflux of cholesterol and phospholipid from cells to extracellular apo, preventing a build-up of excess cholesterol in membranes. This process generates HDL particles that perform a variety of functions to protect against disease. A number of these functions can be viewed as directly or indirectly supporting ABCA1 activity, thus constituting a positive feedback system to optimize cellular lipid efflux responses and disease prevention. Consequently, therapeutic approaches that mimic the activities of apos may prove highly effective to combat disease. One such approach involves the use of peptides. The broad biological relevance of ABCA1 suggests these apo mimetic peptides may be useful for the treatment of a number of diseases, such as atherosclerosis, diabetes, and Alzheimer's disease.
机译：综述的目的该综述总结了与刺激细胞胆固醇外排的新型载脂蛋白（apo）E模拟肽的临床前开发有关的信息。最近发现基于apoE C末端结构域的小螺旋肽已被开发用于治疗应用。这些肽通过ATP结合盒转运蛋白A1（ABCA1）高效刺激细胞胆固醇外排，就像天然的载脂蛋白一样，以摩尔为基础。这种有效的活性与这些肽在稀释时保持-螺旋结构的独特能力有关。最近的结构活性研究改善了这些模拟肽的安全性，极大地提高了其临床应用潜力。这些研究已经确定了诱导肌肉毒性和高甘油三酯血症的A类螺旋基序的结构特征，这可能对其他HDL模拟肽的设计有影响.SummaryABCA1是一种在生物学中起着核心作用的不可或缺的膜蛋白。它的主要功能是介导胆固醇和磷脂从细胞到细胞外载脂蛋白的外排，防止膜中多余胆固醇的积聚。该过程产生HDL颗粒，这些颗粒具有多种功能来预防疾病。可以将这些功能中的许多功能视为直接或间接支持ABCA1活性，从而构成一个正反馈系统，以优化细胞脂质外流反应和疾病预防。因此，模仿‘a’活性的治疗方法可证明对疾病有效。一种这样的方法涉及使用肽。 ABCA1具有广泛的生物学意义，表明这些载脂蛋白模拟肽可能可用于治疗多种疾病，例如动脉粥样硬化，糖尿病和阿尔茨海默氏病。

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