Geng Yanyan, Liu Changdong, Miao Haitao, Suen Monica Ching, Xie Yuanyuan, Zhang Bingchang, Han Wanhong, Wu Caiming, Ren Haixia, Chen Xueqin, Tai Hwan-Ching, Wang Zhanxiang, Zhu Guang, Cai Qixu
Clinical Research Institute of the First Affiliated Hospital of Xiamen University, Fujian Key Laboratory of Brain Tumors Diagnosis and Precision Treatment, Xiamen Key Laboratory of Brain Center, the First Affiliated Hospital of Xiamen University, School of Public Health, School of Medicine, Xiamen University, Xiamen 361003, Fujian, China.
Institute for Advanced Study and State Key Laboratory of Molecular Neuroscience, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China.
Nucleic Acids Res. 2025 Sep 5;53(17). doi: 10.1093/nar/gkaf879.
The abnormal expansion of GGGGCC (G4C2) repeats in the noncoding region of the C9orf72 gene is a major genetic cause of two devastating neurodegenerative disorders, amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). These G4C2 repeats are known to form G-quadruplex (G4) structures, which are hypothesized to contribute to disease pathogenesis. Here, we demonstrated that four DNA G4C2 repeats can fold into two structurally distinct G4 conformations: a parallel and an antiparallel topology. The high-resolution crystal structure of the parallel G4 reveals an eight-layered dimeric assembly, formed by two identical monomeric units. Each unit contains four stacked G-tetrads connected by three propeller CC loops and is stabilized through 5'-to-5' π-π interactions and coordination with a central K+ ion. Notably, the 3'-ending cytosines form a C·C+·C·C+ quadruple base pair stacking onto the adjacent G-tetrad layer. In contrast, the antiparallel G4 adopts a four-layered monomeric structure with three edgewise loops, where the C6 and C18 bases engage in stacking interaction with neighboring G-tetrad via a K+ ion. These structurally distinct G-quadruplexes provide mechanistic insights into C9orf72-associated neurodegeneration and offer potential targets for the development of structure-based therapeutic strategies for ALS and FTD.
C9orf72基因非编码区中GGGGCC(G4C2)重复序列的异常扩增是两种毁灭性神经退行性疾病——肌萎缩侧索硬化症(ALS)和额颞叶痴呆(FTD)的主要遗传病因。已知这些G4C2重复序列会形成G-四链体(G4)结构,据推测该结构与疾病发病机制有关。在此,我们证明四个DNA G4C2重复序列可折叠成两种结构不同的G4构象:平行拓扑结构和反平行拓扑结构。平行G4的高分辨率晶体结构揭示了一种由两个相同单体单元形成的八层二聚体组装体。每个单元包含四个由三个螺旋桨状CC环连接的堆叠G-四联体,并通过5'至5'的π-π相互作用以及与中心K+离子的配位作用得以稳定。值得注意的是,3'末端的胞嘧啶形成了一个C·C+·C·C+四重碱基对,堆叠在相邻的G-四联体层上。相比之下,反平行G4采用具有三个边缘环的四层单体结构,其中C6和C18碱基通过K+离子与相邻的G-四联体进行堆叠相互作用。这些结构不同的G-四链体为C9orf72相关神经退行性变提供了机制性见解,并为开发基于结构的ALS和FTD治疗策略提供了潜在靶点。