Department of Structural Biology, Weizmann Institute of Science, Rehovot 76100, Israel; email:
Annu Rev Biochem. 2017 Jun 20;86:567-583. doi: 10.1146/annurev-biochem-061516-044617.
Multidrug resistance is a global threat as the clinically available potent antibiotic drugs are becoming exceedingly scarce. For example, increasing drug resistance among gram-positive bacteria is responsible for approximately one-third of nosocomial infections. As ribosomes are a major target for these drugs, they may serve as suitable objects for novel development of next-generation antibiotics. Three-dimensional structures of ribosomal particles from Staphylococcus aureus obtained by X-ray crystallography have shed light on fine details of drug binding sites and have revealed unique structural motifs specific for this pathogenic strain, which may be used for the design of novel degradable pathogen-specific, and hence, environmentally friendly drugs.
多药耐药性是一个全球性的威胁,因为临床上可用的强效抗生素药物变得越来越稀缺。例如,革兰氏阳性菌的耐药性增加导致了大约三分之一的医院获得性感染。由于核糖体是这些药物的主要靶标,因此它们可能成为开发下一代抗生素的合适对象。通过 X 射线晶体学获得的金黄色葡萄球菌核糖体颗粒的三维结构揭示了药物结合位点的精细细节,并揭示了这种病原体菌株特有的独特结构基序,可用于设计新型的可降解的、针对病原体的、因此对环境友好的药物。