NanoScience Technology Center, University of Central Florida, 12424 Research Parkway, Suite 400, Orlando, FL 32826, USA.
Burnett School of Biomedical Sciences, College of Medicine, University of Central Florida, Orlando, FL 32816, USA.
Int J Mol Sci. 2023 Aug 31;24(17):13519. doi: 10.3390/ijms241713519.
Although skeletal muscle (hSKM) has been proven to be actively involved in Amyotrophic Lateral Sclerosis (ALS) neuromuscular junction (NMJ) dysfunction, it is rarely considered as a pharmacological target in preclinical drug discovery. This project investigated how improving ALS hSKM viability and function effects NMJ integrity. Phenotypic ALS NMJ human-on-a-chip models developed from patient-derived induced pluripotent stem cells (iPSCs) were used to study the effect of hSKM-specific creatine treatment on clinically relevant functional ALS NMJ parameters, such as NMJ numbers, fidelity, stability, and fatigue index. Results indicated comparatively enhanced NMJ numbers, fidelity, and stability, as well as reduced fatigue index, across all hSKM-specific creatine-treated systems. Immunocytochemical analysis of the NMJs also revealed improved post-synaptic nicotinic Acetylcholine receptor (AChR) clustering and cluster size in systems supplemented with creatine relative to the un-dosed control. This work strongly suggests hSKM as a therapeutic target in ALS drug discovery. It also demonstrates the need to consider all tissues involved in multi-systemic diseases, such as ALS, in drug discovery efforts. Finally, this work further establishes the BioMEMs NMJ platform as an effective means of performing mutation-specific drug screening, which is a step towards personalized medicine for rare diseases.
尽管骨骼肌(hSKM)已被证明在肌萎缩侧索硬化症(ALS)神经肌肉接点(NMJ)功能障碍中起积极作用,但在临床前药物发现中很少将其视为药理学靶点。本项目研究了改善 ALS hSKM 活力和功能对 NMJ 完整性的影响。使用源自患者衍生的诱导多能干细胞(iPSC)的表型 ALS NMJ 人源芯片模型来研究 hSKM 特异性肌酸治疗对临床相关功能 ALS NMJ 参数的影响,例如 NMJ 数量、保真度、稳定性和疲劳指数。结果表明,与未处理的对照相比,所有 hSKM 特异性肌酸处理系统的 NMJ 数量、保真度和稳定性均得到了相对增强,而疲劳指数则降低了。NMJ 的免疫细胞化学分析还显示,与未处理的对照相比,在补充肌酸的系统中,突触后烟碱型乙酰胆碱受体(AChR)聚集和簇大小得到了改善。这项工作强烈表明 hSKM 是 ALS 药物发现中的一个治疗靶点。它还表明,在药物发现工作中,需要考虑到涉及多系统疾病(如 ALS)的所有组织。最后,这项工作进一步确立了 BioMEMs NMJ 平台作为进行突变特异性药物筛选的有效手段,这是迈向罕见病个体化医疗的一步。