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Review Article

具有抗Prion活性的小分子

卷 27, 期 33, 2020

页: [5446 - 5479] 页: 34

弟呕挨: 10.2174/0929867326666190927121744

价格: $65

摘要

朊蛋白是一种致命的神经退行性疾病，由生理朊蛋白(PrPC)错折叠成一种β结构丰富的异构体，称为PrPSC。 到目前为止，还没有治疗朊病毒疾病的有效方法，只是进行了一些临床试验。 最初的寻找抗Prion药物的方法是以PrPSC为目标，但由于PrPSC的替代构象而产生的不同朊蛋白菌株的存在，限制了配体的有效性，使其具有不依赖的能力。这就使研究转向了通过稳定天然构象或抑制其与PrPSc相互作用而充当分子伴侣的PrPC配体。还研究了过渡金属介导的氧化过程在朊蛋白错折叠中的作用。 另一种有前途的方法是通过其他细胞靶点间接作用，如膜结构域或核糖体的蛋白质折叠活性(PFAR)。 此外，还开发了新的朊蛋白特异性高通量筛选技术。 然而，到目前为止，还没有发现任何物质能够令人满意地延长朊病毒疾病动物模型的生存时间。 本文综述了不同化学类型的抗先验剂的构效关系(SAR)的主要特征。

关键词: 朊病毒，传染性海绵状脑病，瘙痒病，淀粉样蛋白，组织学染料，构效关系(SAR)。

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