NO is an important messenger molecule in the brain, playing an important role in learning and memory, in particular via the ERK/CREB signaling pathway. NO is also a neuroprotective agent; multiple mechanisms having been demonstrated that can contribute to cell survival as levels of antioxidants and trophic factors are reduced with aging. Small molecules that mimic the biological activity of NO, including NO donors, may thus ameliorate cognition and provide neuroprotection. Several lines of evidence have linked the neurodegeneration and dementia characteristic of Alzheimer's disease with the action of beta-amyloid protein at the alpha7-nicotinic acetylcholine receptor. The interplay of Abeta with alpha7-nicotinic ACh receptors operating via the ERK signaling cascade links the amyloid cascade and the cholinergic hypothesis in pathways that impact synaptic plasticity and memory. This interplay also provides linkages to disruption of NO/cGMP signaling in AD, and in addition, recent direct evidence has been found demonstrating that Abeta downregulates the NO/cGMP/CREB pathway. Activation of soluble guanylyl cyclase elevating cGMP in the brain represents the central element of a therapeutic approach to the treatment of AD and other neurodegenerative diseases, furthermore, evidence suggests that NO may display cGMP-independent activity and may operate via multiple biochemical signaling pathways to ensure the survival of neurons subjected to stress. GT 1061 is an NO chimera, an NO mimetic compound that contains an ancillary, synergistic pharmacophore, currently in clinical trials for Alzheimer's. NO chimeras and hybrid nitrates hold promise as therapeutics for AD with multiple sites of action.

译文

NO是大脑中重要的信使分子,在学习和记忆中起着重要作用,尤其是通过ERK/CREB信号通路。NO也是神经保护剂; 已经证明了多种机制可以促进细胞存活,因为随着衰老,抗氧化剂和营养因子的水平降低。模拟NO生物活性的小分子,包括NO供体,可以改善认知并提供神经保护。有几条证据表明,阿尔茨海默氏病的神经变性和痴呆特征与 β-淀粉样蛋白在alpha7-nicotinic乙酰胆碱受体上的作用有关。Abeta与通过ERK信号级联起作用的alpha7-nicotinic ACh受体的相互作用将影响突触可塑性和记忆的途径中的淀粉样蛋白级联反应和胆碱能假说联系起来。这种相互作用还提供了与AD中NO/cGMP信号传导中断的联系,此外,最近发现的直接证据表明Abeta下调了NO/cGMP/CREB途径。可溶性鸟苷酸环化酶的激活升高了大脑中的cGMP,代表了治疗AD和其他神经退行性疾病的治疗方法的核心要素,此外,有证据表明NO可能显示出不依赖cGMP的活性,并且可以通过多种生化信号传导途径起作用,以确保承受压力的神经元的存活。GT 1061是一种NO嵌合体,一种NO模拟化合物,包含辅助的,协同药效团,目前正在阿尔茨海默氏症的临床试验中。没有嵌合体和杂合硝酸盐有望作为具有多个作用位点的AD的治疗方法。

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