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NMNAT2 是一个可成药的靶点,可促进神经元 NAD 产生。

NMNAT2 is a druggable target to drive neuronal NAD production.

机构信息

Department of Clinical Neuroscience, Division of Eye and Vision, St. Erik Eye Hospital; Karolinska Institutet, Stockholm, Sweden.

School of Pharmacy and Pharmaceutical Sciences; Cardiff University, Cardiff, Wales, UK.

出版信息

Nat Commun. 2024 Jul 24;15(1):6256. doi: 10.1038/s41467-024-50354-5.

Abstract

Maintenance of NAD pools is critical for neuronal survival. The capacity to maintain NAD pools declines in neurodegenerative disease. We identify that low NMNAT2, the critical neuronal NAD producing enzyme, drives retinal susceptibility to neurodegenerative insults. As proof of concept, gene therapy over-expressing full length human NMNAT2 is neuroprotective. To pharmacologically target NMNAT2, we identify that epigallocatechin gallate (EGCG) can drive NAD production in neurons through an NMNAT2 and NMN dependent mechanism. We confirm this by pharmacological and genetic inhibition of the NAD-salvage pathway. EGCG is neuroprotective in rodent (mixed sex) and human models of retinal neurodegeneration. As EGCG has poor drug-like qualities, we use it as a tool compound to generate novel small molecules which drive neuronal NAD production and provide neuroprotection. This class of NMNAT2 targeted small molecules could have an important therapeutic impact for neurodegenerative disease following further drug development.

摘要

维持 NAD 池对于神经元的存活至关重要。在神经退行性疾病中,维持 NAD 池的能力会下降。我们发现,关键的神经元 NAD 产生酶 NMNAT2 水平较低,会导致视网膜易受神经退行性损伤的影响。作为概念验证,过表达全长人 NMNAT2 的基因治疗具有神经保护作用。为了对 NMNAT2 进行药物靶向治疗,我们发现表没食子儿茶素没食子酸酯(EGCG)可以通过 NMNAT2 和 NMN 依赖的机制在神经元中驱动 NAD 产生。我们通过抑制 NAD 挽救途径的药理学和遗传学抑制来证实这一点。EGCG 在啮齿动物(混合性别)和人类视网膜神经退行性变模型中具有神经保护作用。由于 EGCG 的药物样性质较差,我们将其用作工具化合物来生成新型小分子,这些小分子可驱动神经元 NAD 产生并提供神经保护。在进一步的药物开发之后,这类针对 NMNAT2 的小分子可能对神经退行性疾病具有重要的治疗影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7d8/11269627/cbeac989ef4a/41467_2024_50354_Fig1_HTML.jpg

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