Department Medical and Molecular Genetics, King's College London School of Medicine, King's College London, London SE1 9RT, United Kingdom.
J Biol Chem. 2010 Mar 19;285(12):8808-23. doi: 10.1074/jbc.M109.075028. Epub 2010 Jan 19.
Huntingtin proteolysis has been implicated in the molecular pathogenesis of Huntington disease (HD). Despite an intense effort, the identity of the pathogenic smallest N-terminal fragment has not been determined. Using a panel of anti-huntingtin antibodies, we employed an unbiased approach to generate proteolytic cleavage maps of mutant and wild-type huntingtin in the HdhQ150 knock-in mouse model of HD. We identified 14 prominent N-terminal fragments, which, in addition to the full-length protein, can be readily detected in cytoplasmic but not nuclear fractions. These fragments were detected at all ages and are not a consequence of the pathogenic process. We demonstrated that the smallest fragment is an exon 1 huntingtin protein, known to contain a potent nuclear export signal. Prior to the onset of behavioral phenotypes, the exon 1 protein, and possibly other small fragments, accumulate in neuronal nuclei in the form of a detergent insoluble complex, visualized as diffuse granular nuclear staining in tissue sections. This methodology can be used to validate the inhibition of specific proteases as therapeutic targets for HD by pharmacological or genetic approaches.
亨廷顿病(HD)的分子发病机制与亨廷顿蛋白的水解有关。尽管进行了大量研究,但致病的最小 N 端片段的身份仍未确定。本研究使用一组抗亨廷顿蛋白抗体,采用一种无偏见的方法,在 HD 的 HdhQ150 基因敲入小鼠模型中生成突变型和野生型亨廷顿蛋白的蛋白水解图谱。我们鉴定了 14 个明显的 N 端片段,除全长蛋白外,这些片段还可以在细胞质而非核部分中轻易检测到。这些片段在所有年龄段都能被检测到,而且不是致病过程的结果。我们证明最小的片段是一个包含有效核输出信号的外显子 1 亨廷顿蛋白。在行为表型出现之前,外显子 1 蛋白,以及可能的其他小片段,以胶溶复合物的形式在神经元核中积累,在组织切片中表现为弥散的颗粒状核染色。这种方法可用于通过药理学或遗传学方法验证特定蛋白酶抑制剂作为 HD 的治疗靶点。