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arXiv 1704.08313physics.bio-ph
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以淀粉样蛋白- \b{eta}为靶点的药物及其给药系统

Drugs and Drug Delivery Systems Targeting Amyloid-\b{eta} in Alzheimers Disease

Morgan Robinson, Brenda Yasie Lee, Zoya Leonenko

摘要:

阿尔茨海默病(AD)是一种毁灭性的神经退行性疾病,无法治愈,并且治疗方案有限,无法针对任何可疑的原因。越来越多的证据表明,神经变性的原因之一是淀粉样蛋白β(A \b{eta})的过度产生和A \b{eta}肽不能从脑中清除,导致自聚集以形成毒性低聚物、原纤维和斑块。潜在的治疗选择之一是靶向A \b{eta}并防止自聚集以允许大脑的自然清除。本文综述了以A \b{eta}为靶点的药物及其给药系统与阿尔茨海默病的关系。已经进行了许多尝试来使用能够靶向A \b{eta}的抗A \b{eta}靶向分子(在体外和体内动物模型中取得了很大成功),但是该技术的主要障碍是血脑屏障(BBB)带来的挑战。这种高度选择性的屏障保护大脑免受有毒分子和病原体的侵害,并阻止大多数药物的输送。因此,新型A \b{eta}聚集抑制剂药物将需要经过深思熟虑的药物递送系统以将足够的浓度递送至脑。

英文摘要:

Alzheimer's disease (AD) is a devastating neurodegenerative disorder with no cure and limited treatment solutions that are unable to target any of the suspected causes. Increasing evidence suggests that one of the causes of neurodegeneration is the overproduction of amyloid beta (A\b{eta}) and the inability of A\b{eta} peptides to be cleared from the brain, resulting in self-aggregation to form toxic oligomers, fibrils and plaques. One of the potential treatment options is to target A\b{eta} and prevent self-aggregation to allow for a natural clearing of the brain. In this paper, we review the drugs and drug delivery systems that target A\b{eta} in relation to Alzheimer's disease. Many attempts have been made to use anti-A\b{eta} targeting molecules capable of targeting A\b{eta} (with much success in vitro and in vivo animal models), but the major obstacle to this technique is the challenge posed by the blood brain barrier (BBB). This highly selective barrier protects the brain from toxic molecules and pathogens and prevents the delivery of most drugs. Therefore novel A\b{eta} aggregation inhibitor drugs will require well thought-out drug delivery systems to deliver sufficient concentrations to the brain.

机构、总结、中文摘要均由AI分析而来,可能存在错误,请以论文正文为准。

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