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Trends Biotechnol. 2010 Dec;28(12):596-604. doi: 10.1016/j.tibtech.2010.09.004. Epub 2010 Oct 21.
Most infections are caused by bacteria, many of which are ever-evolving and resistant to nearly all available antibiotics. β-Lactams and glycopeptides are used to combat these infections by inhibiting bacterial cell-wall synthesis. This mechanism remains an interesting target in the search for new antibiotics in light of failed genomic approaches and the limited input of major pharmaceutical companies. Several strategies have enriched the pipeline of bacterial cell-wall inhibitors; examples include combining screening strategies with lesser-explored microbial diversity, or reinventing known scaffolds based on structure-function relationships. Drugs developed using novel strategies will contribute to the arsenal in fight against the continued emergence of bacterial resistance.
大多数感染是由细菌引起的,其中许多细菌不断进化,对几乎所有可用的抗生素都具有耐药性。β-内酰胺类和糖肽类抗生素通过抑制细菌细胞壁合成来对抗这些感染。鉴于基因组方法的失败和大型制药公司的投入有限,这种机制仍然是寻找新抗生素的一个有趣目标。几种策略丰富了细菌细胞壁抑制剂的研发管线;例如,将筛选策略与较少探索的微生物多样性相结合,或者根据结构-功能关系重新设计已知的支架。使用新策略开发的药物将有助于对抗细菌耐药性的持续出现。