Amicus Therapeutics, 1 Cedar Brook Dr., Cranbury, NJ 08512, United States.
Amicus Therapeutics, 1 Cedar Brook Dr., Cranbury, NJ 08512, United States.
Bioorg Med Chem Lett. 2014 Jul 15;24(14):3001-5. doi: 10.1016/j.bmcl.2014.04.108. Epub 2014 May 14.
Mutations in the gene that encodes the lysosomal enzyme acid β-glucosidase lead to reduced cellular activity and accumulation of glycosphingolipid substrates, biochemical hallmarks of the lysosomal storage disorder Gaucher disease (GD). Recently such mutations have been identified as risk factors for Parkinson's disease (PD) and related disorders. Both gain-of-function (due to toxic cellular accumulation of mutant enzyme) and loss-of-function (due to accumulation of lipid substrates) hypotheses have been put forth to address the biochemical link between GD and PD. Similarly, links between Alzheimer's disease and other lysosomal enzyme deficiencies have begun to emerge. The use of pharmacological chaperones to restore the cellular trafficking and activity of mutant lysosomal enzymes may offer a novel approach to treat these debilitating neurodegenerative diseases.
基因突变导致溶酶体酶酸性β-葡萄糖苷酶的编码基因,导致细胞活性降低和糖脂底物的积累,这是溶酶体贮积病 Gaucher 病(GD)的生化标志。最近,这些突变被确定为帕金森病(PD)和相关疾病的危险因素。两种假说都提出了功能获得(由于突变酶的细胞毒性积累)和功能丧失(由于脂质底物的积累),以解决 GD 和 PD 之间的生化联系。同样,阿尔茨海默病与其他溶酶体酶缺乏之间的联系也开始显现。使用药理学伴侣来恢复突变溶酶体酶的细胞运输和活性,可能为治疗这些使人衰弱的神经退行性疾病提供一种新方法。