{"title":"阿尔茨海默病的最新进展:机制、临床试验和新药开发战略。","authors":"Jifa Zhang, Yinglu Zhang, Jiaxing Wang, Yilin Xia, Jiaxian Zhang, Lei Chen","doi":"10.1038/s41392-024-01911-3","DOIUrl":null,"url":null,"abstract":"<p><p>Alzheimer's disease (AD) stands as the predominant form of dementia, presenting significant and escalating global challenges. Its etiology is intricate and diverse, stemming from a combination of factors such as aging, genetics, and environment. Our current understanding of AD pathologies involves various hypotheses, such as the cholinergic, amyloid, tau protein, inflammatory, oxidative stress, metal ion, glutamate excitotoxicity, microbiota-gut-brain axis, and abnormal autophagy. Nonetheless, unraveling the interplay among these pathological aspects and pinpointing the primary initiators of AD require further elucidation and validation. In the past decades, most clinical drugs have been discontinued due to limited effectiveness or adverse effects. Presently, available drugs primarily offer symptomatic relief and often accompanied by undesirable side effects. However, recent approvals of aducanumab (1) and lecanemab (2) by the Food and Drug Administration (FDA) present the potential in disrease-modifying effects. Nevertheless, the long-term efficacy and safety of these drugs need further validation. Consequently, the quest for safer and more effective AD drugs persists as a formidable and pressing task. This review discusses the current understanding of AD pathogenesis, advances in diagnostic biomarkers, the latest updates of clinical trials, and emerging technologies for AD drug development. We highlight recent progress in the discovery of selective inhibitors, dual-target inhibitors, allosteric modulators, covalent inhibitors, proteolysis-targeting chimeras (PROTACs), and protein-protein interaction (PPI) modulators. 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引用次数: 0
摘要
阿尔茨海默病(AD)是痴呆症的主要形式,给全球带来了不断升级的重大挑战。它的病因复杂多样,源于衰老、遗传和环境等综合因素。我们目前对痴呆症病理的理解涉及多种假说,如胆碱能、淀粉样蛋白、tau 蛋白、炎症、氧化应激、金属离子、谷氨酸兴奋毒性、微生物群-肠-脑轴和异常自噬等。尽管如此,要揭示这些病理因素之间的相互影响,并精确定位AD的主要诱发因素,还需要进一步的阐明和验证。在过去几十年中,大多数临床药物都因疗效有限或不良反应而停用。目前,现有药物主要缓解症状,但往往伴有不良副作用。不过,美国食品药品管理局(FDA)最近批准了阿杜卡单抗(1)和莱卡内单抗(2),这两种药物具有缓解病情的潜在作用。然而,这些药物的长期疗效和安全性还需要进一步验证。因此,寻求更安全、更有效的 AD 药物仍然是一项艰巨而紧迫的任务。本综述讨论了目前对注意力缺失症发病机制的认识、诊断生物标志物的进展、临床试验的最新进展以及用于注意力缺失症药物开发的新兴技术。我们重点介绍了在发现选择性抑制剂、双靶点抑制剂、异位调节剂、共价抑制剂、蛋白水解靶向嵌合体(PROTACs)和蛋白-蛋白相互作用(PPI)调节剂方面的最新进展。我们的目标是为新型抗抑郁药物的前瞻性开发和临床应用提供真知灼见。
Recent advances in Alzheimer's disease: Mechanisms, clinical trials and new drug development strategies.
Alzheimer's disease (AD) stands as the predominant form of dementia, presenting significant and escalating global challenges. Its etiology is intricate and diverse, stemming from a combination of factors such as aging, genetics, and environment. Our current understanding of AD pathologies involves various hypotheses, such as the cholinergic, amyloid, tau protein, inflammatory, oxidative stress, metal ion, glutamate excitotoxicity, microbiota-gut-brain axis, and abnormal autophagy. Nonetheless, unraveling the interplay among these pathological aspects and pinpointing the primary initiators of AD require further elucidation and validation. In the past decades, most clinical drugs have been discontinued due to limited effectiveness or adverse effects. Presently, available drugs primarily offer symptomatic relief and often accompanied by undesirable side effects. However, recent approvals of aducanumab (1) and lecanemab (2) by the Food and Drug Administration (FDA) present the potential in disrease-modifying effects. Nevertheless, the long-term efficacy and safety of these drugs need further validation. Consequently, the quest for safer and more effective AD drugs persists as a formidable and pressing task. This review discusses the current understanding of AD pathogenesis, advances in diagnostic biomarkers, the latest updates of clinical trials, and emerging technologies for AD drug development. We highlight recent progress in the discovery of selective inhibitors, dual-target inhibitors, allosteric modulators, covalent inhibitors, proteolysis-targeting chimeras (PROTACs), and protein-protein interaction (PPI) modulators. Our goal is to provide insights into the prospective development and clinical application of novel AD drugs.
期刊介绍:
Signal Transduction and Targeted Therapy is an open access journal that focuses on timely publication of cutting-edge discoveries and advancements in basic science and clinical research related to signal transduction and targeted therapy.
Scope: The journal covers research on major human diseases, including, but not limited to:
Cancer,Cardiovascular diseases,Autoimmune diseases,Nervous system diseases.