Couturier M, Van Melderen L
Dépt de Biologie Moléculaire, Université Libre de Bruxelles, Rhode-Saint-Genèse, Belgium.
Trends Microbiol. 1998 Jul;6(7):269-75. doi: 10.1016/s0966-842x(98)01311-0.
DNA gyrase is an essential topoisomerase that is found in all bacteria and is the target of potent antibiotics, such as the quinolones. By creating DNA lesions and inducing the bacterial SOS response, these drugs are not only highly cytotoxic but also mutagenic. Discovery and analysis of natural molecules with anti-gyrase activities, such as the CcdB or microcin B17 proteins, hold promise for understanding further topoisomerase reactions and for the design of new antibiotics.
DNA促旋酶是一种存在于所有细菌中的必需拓扑异构酶,是喹诺酮类等强效抗生素的作用靶点。通过造成DNA损伤并诱导细菌的SOS反应,这些药物不仅具有高度细胞毒性,而且具有致突变性。发现和分析具有抗促旋酶活性的天然分子,如CcdB或微小菌素B17蛋白,有望进一步了解拓扑异构酶反应并设计新的抗生素。