Rosenblum Lauren Taylor, Trotti Davide
Jefferson Weinberg ALS Center, Vickie and Jack Farber Institute for Neuroscience, Department of Neuroscience, Thomas Jefferson University, 900 Walnut St, Philadelphia, PA, 19107, USA.
Adv Neurobiol. 2017;16:117-136. doi: 10.1007/978-3-319-55769-4_6.
Amyotrophic lateral sclerosis (ALS) is a rapid and fatal neurodegenerative disease, primarily affecting upper and lower motor neurons. It is an extremely heterogeneous disease in both cause and symptom development, and its mechanisms of pathogenesis remain largely unknown. Excitotoxicity, a process caused by excessive glutamate signaling, is believed to play a substantial role, however. Excessive glutamate release, changes in postsynaptic glutamate receptors, and reduction of functional astrocytic glutamate transporters contribute to excitotoxicity in ALS. Here, we explore the roles of each, with a particular emphasis on glutamate transporters and attempts to increase them as therapy for ALS. Screening strategies have been employed to find compounds that increase the functional excitatory amino acid transporter EAAT2 (GLT1), which is responsible for the vast majority of glutamate clearance. One such compound, ceftriaxone, was recently tested in clinical trials but unfortunately did not modify disease course, though its effect on EAAT2 expression in patients was not measured.
肌萎缩侧索硬化症(ALS)是一种快速进展且致命的神经退行性疾病,主要影响上下运动神经元。它在病因和症状发展方面都是一种极其异质性的疾病,其发病机制在很大程度上仍不清楚。然而,由过量谷氨酸信号传导引起的兴奋毒性被认为起着重要作用。过量的谷氨酸释放、突触后谷氨酸受体的变化以及功能性星形胶质细胞谷氨酸转运体的减少都导致了ALS中的兴奋毒性。在此,我们探讨了它们各自的作用,特别强调了谷氨酸转运体,并尝试增加其表达作为ALS的治疗方法。已经采用筛选策略来寻找能增加功能性兴奋性氨基酸转运体EAAT2(GLT1)的化合物,该转运体负责绝大多数谷氨酸的清除。一种这样的化合物头孢曲松最近在临床试验中进行了测试,但遗憾的是并没有改变疾病进程,尽管未测量其对患者中EAAT2表达的影响。