RNA Systems Biochemistry Laboratory, RIKEN Cluster for Pioneering Research, Wako, Saitama, 351-0198, Japan.
RNA Systems Biochemistry Laboratory, RIKEN Cluster for Pioneering Research, Wako, Saitama, 351-0198, Japan; Department of Computational Biology and Medical Sciences, Graduate School of Frontier Sciences, The University of Tokyo, Kashiwa, Chiba, 277-8561, Japan.
Curr Opin Chem Biol. 2022 Aug;69:102158. doi: 10.1016/j.cbpa.2022.102158. Epub 2022 May 19.
Since many human diseases are caused by the unwelcome production of harmful proteins, compounds that selectively suppress protein synthesis should provide a unique path for drug development, expanding the druggable proteome. Although surveying the RNA/amino acid contexts that are preferentially affected by translation inhibitors has presented an analytic hurdle, the application of a technique termed ribosome profiling overcomes this problem. Indeed, this technique uncovers the selectivity of translation repression by small molecules such as chloramphenicol, macrolides, PF846, and rocaglates. The molecular understanding of how the compounds inspire context selectivity, despite their targeting to general translation machinery, facilitates rational drug design and discovery for therapeutic purposes.
由于许多人类疾病是由有害蛋白质的不受欢迎产生引起的,因此选择性抑制蛋白质合成的化合物应该为药物开发提供一条独特的途径,从而扩大可用药蛋白组。尽管调查受翻译抑制剂优先影响的 RNA/氨基酸环境提出了一个分析上的障碍,但一种称为核糖体分析的技术的应用克服了这个问题。事实上,这项技术揭示了小分子如氯霉素、大环内酯类、PF846 和罗卡利特等对翻译抑制的选择性。尽管这些化合物的作用靶点是一般的翻译机制,但它们如何激发上下文选择性的分子理解,有助于为治疗目的进行合理的药物设计和发现。