核糖开关——药物开发的新靶点

核糖开关——药物开发的新靶点 Riboswitches:New Targets for Drug Discovery 刘湛军 LIU Zhanjun 1 first-author 路新枝 LU Xinzhi 1 姜鹏 JIANG Peng 1 于文功 YU Wengong 1 中国海洋大学医药学院 中国海洋大学医药学院 School of Medicine and Pharmacy,Ocean University of China School of Medicine and Pharmacy,Ocean University of China 核糖开关是mRNA上能够与自由代谢产物或其他小分子配体结合或由于环境条件变化而引起构象变化从而调控基因表达的RNA结构元件.核糖开关广泛存在于G+及G-细菌代谢相关基因中,在真菌、植物和高等动物人的血管内皮生长因子基因中也有发现.核糖开关控制生物体内许多重要基因的表达,调节体内基础代谢,信号传递以及氨基酸、核苷酸、辅酶、金属离子的摄取.核糖开关在生物代谢调控、信号传导中的重要作用使其成为一类新型的药物作用靶点,为新型抗生素研发开辟了新的领域.本文综述了核糖开关的研究进展、作用机制、结构功能以及其在开发新型药物方面的研究策略. Riboswitches are metabolite-binding RNA elements that serve as gene regulatory elements through conformation change when small ligand bands or environment changes.Riboswitches are widely distributed in Gram positive and negative bacterium metabolite genes,and also was found in fungi,plants and human vascular endothelial growth factor.Riboswitches control a broad range of genes in bacterial species,including those involved in metabolism,signal conduction or uptake of amino acids,nucleotides,cofactors and metal ions.Their important function in microbial metabolic regulation and signal conduction make them as novel drug targets for developing new antibacterials.In this review,we will give an overview of riboswitches in current progresses,mechanism,structure and function as well as the research strategy in new drug development. 核糖开关 基因表达调控 药物靶点 riboswitch gene expression regulation drug targets 10.14188/j.1671-8836.2010.03.001 Q52 国家高技术研究发展计划（863计划）重点项目（2007AA091506） 2010-03-01 2021-04-01 3 56