Hermann Thomas
Department of Structural Chemistry, Anadys Pharmaceuticals Inc, 3115 Merryfield Row, San Diego, CA 92121, USA.
Curr Opin Struct Biol. 2005 Jun;15(3):355-66. doi: 10.1016/j.sbi.2005.05.001.
Several classes of clinically important antibiotics target the bacterial ribosome, where they interfere with microbial protein synthesis. Structural studies of the interaction of antibiotics with the ribosome have revealed that these small molecules recognize predominantly the rRNA components. Over the past two years, three-dimensional structures of ribosome-antibiotic complexes have been determined, providing a detailed picture of the binding sites and mechanism of action of antibacterials, including 'blockbuster' drugs such as the macrolides. Structure-based approaches have come to fruition that comprise the design and crystal structure analysis of novel semi-synthetic antibiotics that target the ribosome decoding site.
几类具有临床重要性的抗生素作用于细菌核糖体，干扰微生物蛋白质合成。抗生素与核糖体相互作用的结构研究表明，这些小分子主要识别rRNA组分。在过去两年中，已确定了核糖体 - 抗生素复合物的三维结构，详细描绘了抗菌药物（包括大环内酯类等“重磅炸弹”药物）的结合位点和作用机制。基于结构的方法已经取得成果，包括针对核糖体解码位点的新型半合成抗生素的设计和晶体结构分析。
