Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, Pavia, Italy.
Federal Research Centre "Fundamentals of Biotechnology" of the Russian Academy of Sciences, Moscow, Russia.
Eur J Med Chem. 2020 Mar 15;190:112132. doi: 10.1016/j.ejmech.2020.112132. Epub 2020 Feb 8.
Cystic fibrosis is a rare genetic disease characterized by the production of dehydrated mucus in the lung able to trap bacteria and rendering their proliferation particularly dangerous, thus leading to chronic infections. Among these bacteria, Staphylococcus aureus and Pseudomonas aeruginosa play a major role while, within emerging pathogens, Stenotrophomonas maltophilia, Achromobacter xylosoxidans, Burkholderia cepacia complex species, as well as non-tuberculous mycobacteria are listed. Since a common feature of these bacteria is the high level of drug resistance, cell division, and in particular FtsZ, has been explored as a novel therapeutic target for the design of new molecules with antibacterial properties. This review summarizes and provides insight into recent advances in the discovery of compounds targeting FtsZ: the majority of them exhibit anti-staphylococcal activity, while a few were directed against the cystic fibrosis Gram negative pathogens.
囊性纤维化是一种罕见的遗传性疾病,其特征是肺部产生脱水的黏液,能够捕捉细菌并使其增殖变得特别危险,从而导致慢性感染。在这些细菌中,金黄色葡萄球菌和铜绿假单胞菌起着重要作用,而在新兴病原体中,嗜麦芽寡养单胞菌、木糖氧化无色杆菌、洋葱伯克霍尔德菌复合体以及非结核分枝杆菌也被列入其中。由于这些细菌的一个共同特征是高水平的耐药性,因此细胞分裂,特别是 FtsZ,已被探索作为设计具有抗菌特性的新分子的新的治疗靶点。本综述总结并深入探讨了靶向 FtsZ 的化合物的最新发现:它们中的大多数表现出抗葡萄球菌活性,而少数则针对囊性纤维化革兰氏阴性病原体。