Department of Chemistry, Duke University, Durham, North Carolina 27708, United States.
ACS Chem Neurosci. 2021 Nov 3;12(21):3972-3984. doi: 10.1021/acschemneuro.1c00524. Epub 2021 Oct 15.
Disrupted cellular trafficking and transport processes are hallmarks of many neurodegenerative disorders (NDs). Recently, efforts have been made toward developing and implementing experimental platforms to identify small molecules that may help restore normative trafficking functions. There have been a number of successes in targeting endomembrane trafficking with the identification of compounds that restore cell viability through rescue of protein transport and trafficking. Here, we describe some of the experimental platforms implemented for small molecule screening efforts for rescue of trafficking defects in neurodegeneration. A survey of phenotypically active small molecules identified to date is provided, including a summary of medicinal chemistry efforts and insights into putative targets and mechanisms of action. In particular, emphasis is put on ligands that demonstrate activity in more than one model of neurodegeneration as retention of phenotypic activity across ND models suggests conservation of biological targets across NDs.
细胞内运输和转运过程的紊乱是许多神经退行性疾病(NDs)的特征。最近,人们致力于开发和实施实验平台,以鉴定可能有助于恢复正常运输功能的小分子。通过恢复蛋白质运输和转运来挽救细胞活力,已经有许多靶向细胞内膜运输的成功案例。在这里,我们描述了一些用于筛选小分子以恢复神经退行性变中运输缺陷的实验平台。提供了迄今为止已鉴定出的表型活性小分子的调查结果,包括对药物化学研究的总结以及对潜在靶标和作用机制的深入了解。特别是,重点介绍了在多种神经退行性变模型中均具有活性的配体,因为 ND 模型中保留表型活性表明生物靶标在 ND 中具有保守性。