Düchs Matthias, Blazevic Dragica, Rechtsteiner Philipp, Kenny Cynthia, Lamla Thorsten, Low Sarah, Savistchenko Jimmy, Neumann Manuela, Melki Ronald, Schönberger Tanja, Stierstorfer Birgit, Wyatt David, Igney Frederik, Ciossek Thomas
Boehringer Ingelheim Pharma GmbH & Co KG, Biberach an der Riss, Germany.
Boehringer Ingelheim USA, Ridgefield, CT, USA.
NPJ Parkinsons Dis. 2023 Jun 15;9(1):91. doi: 10.1038/s41531-023-00542-9.
Prion-like transmission of pathology in α-synucleinopathies like Parkinson's disease or multiple system atrophy is increasingly recognized as one potential mechanism to address disease progression. Active and passive immunotherapies targeting insoluble, aggregated α-synuclein are already being actively explored in the clinic with mixed outcomes so far. Here, we report the identification of 306C7B3, a highly selective, aggregate-specific α-synuclein antibody with picomolar affinity devoid of binding to the monomeric, physiologic protein. 306C7B3 binding is Ser129-phosphorylation independent and shows high affinity to several different aggregated α-synuclein polymorphs, increasing the likelihood that it can also bind to the pathological seeds assumed to drive disease progression in patients. In support of this, highly selective binding to pathological aggregates in postmortem brains of MSA patients was demonstrated, with no staining in samples from other human neurodegenerative diseases. To achieve CNS exposure of 306C7B3, an adeno-associated virus (AAV) based approach driving expression of the secreted antibody within the brain of (Thy-1)-[A30P]-hα-synuclein mice was used. Widespread central transduction after intrastriatal inoculation was ensured by using the AAV2HBKO serotype, with transduction being spread to areas far away from the inoculation site. Treatment of (Thy-1)-[A30P]-hα-synuclein mice at the age of 12 months demonstrated significantly increased survival, with 306C7B3 concentration reaching 3.9 nM in the cerebrospinal fluid. These results suggest that AAV-mediated expression of 306C7B3, targeting extracellular, presumably disease-propagating aggregates of α-synuclein, has great potential as a disease-modifying therapy for α-synucleinopathies as it ensures CNS exposure of the antibody, thereby mitigating the selective permeability of the blood-brain barrier.
在帕金森病或多系统萎缩等α-突触核蛋白病中,病理的朊病毒样传播日益被认为是一种应对疾病进展的潜在机制。目前,针对不溶性、聚集性α-突触核蛋白的主动和被动免疫疗法正在临床上积极探索,到目前为止结果不一。在此,我们报告了306C7B3的鉴定,这是一种高度选择性、聚集特异性的α-突触核蛋白抗体,具有皮摩尔亲和力,不与单体生理性蛋白结合。306C7B3的结合不依赖于Ser129磷酸化,对几种不同的聚集性α-突触核蛋白多聚体具有高亲和力,增加了它也能结合假定驱动患者疾病进展的病理种子的可能性。为此提供支持的是,已证明其对多系统萎缩患者死后大脑中的病理聚集体具有高度选择性结合,而在其他人类神经退行性疾病的样本中无染色。为了使306C7B3能够进入中枢神经系统,采用了一种基于腺相关病毒(AAV)的方法,驱动分泌抗体在(Thy-1)-[A30P]-人α-突触核蛋白小鼠脑内表达。通过使用AAV2HBKO血清型确保纹状体内接种后广泛的中枢转导,转导扩散到远离接种部位的区域。对12个月大的(Thy-1)-[A30P]-人α-突触核蛋白小鼠进行治疗,结果显示存活率显著提高,脑脊液中306C7B3浓度达到3.9 nM。这些结果表明,AAV介导的306C7B3表达靶向细胞外、可能传播疾病的α-突触核蛋白聚集体,作为一种针对α-突触核蛋白病的疾病修饰疗法具有巨大潜力,因为它确保了抗体进入中枢神经系统,从而减轻了血脑屏障的选择性通透性。